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75747-14-7,MFCD04973892
Catalog No.:AA005ICD

75747-14-7 | 17-AAG

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Purity
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1mg
98%
in stock  
$19.00   $14.00
- +
25mg
98%
in stock  
$268.00   $188.00
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100mg
98%
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$588.00   $412.00
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  • Technical Information
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA005ICD
Chemical Name:
17-AAG
CAS Number:
75747-14-7
Molecular Formula:
C31H43N3O8
Molecular Weight:
585.6884
MDL Number:
MFCD04973892
SMILES:
C=CCNC1=C2C[C@@H](C)C[C@H](OC)[C@H](O)[C@@H](C)/C=C(\C)/[C@@H]([C@H](C=CC=C(C(=O)NC(=CC1=O)C2=O)C)OC)OC(=O)N
NSC Number:
330507
Properties
Properties
 
BP:
797.8°C at 760 mmHg  
Form:
Solid  
MP:
>194°C (dec.)  
Storage:
Keep in dry area;-20 ℃;  

Computed Properties
 
Complexity:
1210  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
6  
Defined Bond Stereocenter Count:
3  
Heavy Atom Count:
42  
Hydrogen Bond Acceptor Count:
9  
Hydrogen Bond Donor Count:
4  
Rotatable Bond Count:
7  
XLogP3:
2.6  

Literature

Title: Exome sequencing of hepatocellular carcinomas identifies new mutational signatures and potential therapeutic targets.

Journal: Nature genetics 20150501

Title: Two novel ALK mutations mediate acquired resistance to the next-generation ALK inhibitor alectinib.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20141115

Title: Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors.

Journal: European journal of medicinal chemistry 20141006

Title: A phase I study of the HSP90 inhibitor retaspimycin hydrochloride (IPI-504) in patients with gastrointestinal stromal tumors or soft-tissue sarcomas.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20131101

Title: Molecular markers for novel therapeutic strategies in pancreatic endocrine tumors.

Journal: Pancreas 20130401

Title: Inhibition of rapamycin-induced Akt phosphorylation by cotylenin A correlates with their synergistic growth inhibition of cancer cells.

Journal: International journal of oncology 20130201

Title: Lapatinib and 17AAG reduce 89Zr-trastuzumab-F(ab')2 uptake in SKBR3 tumor xenografts.

Journal: Molecular pharmaceutics 20121105

Title: Increased expression of heat shock protein 90 under chemical hypoxic conditions protects cardiomyocytes against injury induced by serum and glucose deprivation.

Journal: International journal of molecular medicine 20121101

Title: Pharmacokinetic study of 3-in-1 poly(ethylene glycol)-block-poly(D, L-lactic acid) micelles carrying paclitaxel, 17-allylamino-17-demethoxygeldanamycin, and rapamycin.

Journal: Journal of controlled release : official journal of the Controlled Release Society 20121010

Title: HSP90 inhibition results in apoptosis of Philadelphia acute lymphoblastic leukaemia cells: an attractive prospect of new targeted agents.

Journal: Journal of cancer research and clinical oncology 20121001

Title: 17-allylamino-17-(demethoxy)geldanamycin (17-AAG) is a potent and effective inhibitor of human cytomegalovirus replication in primary fibroblast cells.

Journal: Archives of virology 20121001

Title: Antitumor activity of Triolimus: a novel multidrug-loaded micelle containing Paclitaxel, Rapamycin, and 17-AAG.

Journal: Molecular cancer therapeutics 20121001

Title: Ganetespib (STA-9090), a nongeldanamycin HSP90 inhibitor, has potent antitumor activity in in vitro and in vivo models of non-small cell lung cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20120915

Title: EC144 is a potent inhibitor of the heat shock protein 90.

Journal: Journal of medicinal chemistry 20120913

Title: Multiple kinase pathways involved in the different de novo sensitivity of pancreatic cancer cell lines to 17-AAG.

Journal: The Journal of surgical research 20120701

Title: 17-Allylamino-17-demethoxygeldanamycin and ritonavir inhibit renal cancer growth by inhibiting the expression of heat shock factor-1.

Journal: International journal of oncology 20120701

Title: Inhibition of thymidine phosphorylase expression by using an HSP90 inhibitor potentiates the cytotoxic effect of cisplatin in non-small-cell lung cancer cells.

Journal: Biochemical pharmacology 20120701

Title: Isoxazolo(aza)naphthoquinones: a new class of cytotoxic Hsp90 inhibitors.

Journal: European journal of medicinal chemistry 20120701

Title: Evidence for efficacy of new Hsp90 inhibitors revealed by ex vivo culture of human prostate tumors.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20120701

Title: 17-AAG mediated targeting of Hsp90 limits tert activity in peritoneal sarcoma related malignant ascites by downregulating cyclin D1 during cell cycle entry.

Journal: Experimental oncology 20120701

Title: Inhibition of the mTORC2 and chaperone pathways to treat leukemia.

Journal: Blood 20120621

Title: Hsp90 regulates O-linked β-N-acetylglucosamine transferase: a novel mechanism of modulation of protein O-linked β-N-acetylglucosamine modification in endothelial cells.

Journal: American journal of physiology. Cell physiology 20120615

Title: Blockade of XBP1 splicing by inhibition of IRE1α is a promising therapeutic option in multiple myeloma.

Journal: Blood 20120614

Title: Constitutive AhR activation leads to concomitant ABCG2-mediated multidrug resistance in cisplatin-resistant esophageal carcinoma cells.

Journal: Molecular carcinogenesis 20120601

Title: Expression and therapeutic relevance of heat-shock protein 90 in pancreatic endocrine tumors.

Journal: Endocrine-related cancer 20120601

Title: Folate receptor targeted 17-allylamino-17-demethoxygeldanamycin (17-AAG) loaded polymeric nanoparticles for breast cancer.

Journal: Colloids and surfaces. B, Biointerfaces 20120601

Title: Novel molecular targeted therapies for refractory thyroid cancer.

Journal: Head & neck 20120501

Title: Clinical experience with the heat shock protein-90 inhibitor, tanespimycin, in patients with relapsed lymphoma.

Journal: Leukemia & lymphoma 20120501

Title: Heat shock protein 90 is a promising target for effective growth inhibition of gastrointestinal neuroendocrine tumors.

Journal: International journal of oncology 20120501

Title: Fluorescent protein-labeled glucocorticoid receptor alpha isoform trafficking in cultured human trabecular meshwork cells.

Journal: Investigative ophthalmology & visual science 20120501

Title: Hsp90 interacts specifically with viral RNA and differentially regulates replication initiation of Bamboo mosaic virus and associated satellite RNA.

Journal: PLoS pathogens 20120501

Title: Hsp90 inhibitors and drug resistance in cancer: the potential benefits of combination therapies of Hsp90 inhibitors and other anti-cancer drugs.

Journal: Biochemical pharmacology 20120415

Title: NAD(P)H:quinone oxidoreductase 1 (NQO1) in the sensitivity and resistance to antitumor quinones.

Journal: Biochemical pharmacology 20120415

Title: A phase I trial of docetaxel and pulse-dose 17-allylamino-17-demethoxygeldanamycin in adult patients with solid tumors.

Journal: Cancer chemotherapy and pharmacology 20120401

Title: SUMO-2/3 conjugates accumulating under heat shock or MG132 treatment result largely from new protein synthesis.

Journal: Biochimica et biophysica acta 20120401

Title: Heat shock proteins as key biological targets of the marine natural cyclopeptide perthamide C.

Journal: Molecular bioSystems 20120401

Title: Protein kinase CK2 protects multiple myeloma cells from ER stress-induced apoptosis and from the cytotoxic effect of HSP90 inhibition through regulation of the unfolded protein response.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20120401

Title: Inhibition of p38 MAPK-dependent excision repair cross-complementing 1 expression decreases the DNA repair capacity to sensitize lung cancer cells to etoposide.

Journal: Molecular cancer therapeutics 20120301

Title: Identification of HSP90 as a new GABARAPL1 (GEC1)-interacting protein.

Journal: Biochimie 20120301

Title: Tipifarnib and tanespimycin show synergic proapoptotic activity in U937 cells.

Journal: Journal of cancer research and clinical oncology 20120301

Title: A Phase II trial of 17-allylamino, 17-demethoxygeldanamycin (17-AAG, tanespimycin) in patients with metastatic melanoma.

Journal: Investigational new drugs 20120201

Title: A phase II study of gemcitabine in combination with tanespimycin in advanced epithelial ovarian and primary peritoneal carcinoma.

Journal: Gynecologic oncology 20120201

Title: A phase II study of 17-allylamino-17-demethoxygeldanamycin in metastatic or locally advanced, unresectable breast cancer.

Journal: Breast cancer research and treatment 20120201

Title: Hsp90 inhibitors sensitise human colon cancer cells to topoisomerase I poisons by depletion of key anti-apoptotic and cell cycle checkpoint proteins.

Journal: Biochemical pharmacology 20120201

Title: Ganetespib, a unique triazolone-containing Hsp90 inhibitor, exhibits potent antitumor activity and a superior safety profile for cancer therapy.

Journal: Molecular cancer therapeutics 20120201

Title: Simultaneous inhibition of glutathione- and thioredoxin-dependent metabolism is necessary to potentiate 17AAG-induced cancer cell killing via oxidative stress.

Journal: Free radical biology & medicine 20120115

Title: In vitro assessment of cytochrome P450 inhibition and induction potential of tanespimycin and its major metabolite, 17-amino-17-demethoxygeldanamycin.

Journal: Cancer chemotherapy and pharmacology 20120101

Title: Cooperative enhancement of radiosensitivity after combined treatment of 17-(allylamino)-17-demethoxygeldanamycin and celecoxib in human lung and colon cancer cell lines.

Journal: DNA and cell biology 20120101

Title: In vitro drug treatments reduce the deleterious effects of aggregates containing polyAla expanded PHOX2B proteins.

Journal: Neurobiology of disease 20120101

Title: Cellular growth kinetics distinguish a cyclophilin inhibitor from an HSP90 inhibitor as a selective inhibitor of hepatitis C virus.

Journal: PloS one 20120101

Title: The aggregation and neurotoxicity of TDP-43 and its ALS-associated 25 kDa fragment are differentially affected by molecular chaperones in Drosophila.

Journal: PloS one 20120101

Title: Advances in establishment and analysis of three-dimensional tumor spheroid-based functional assays for target validation and drug evaluation.

Journal: BMC biology 20120101

Title: Effects of HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin (17-AAG) on NEU/HER2 overexpressing mammary tumours in MMTV-NEU-NT mice monitored by Magnetic Resonance Spectroscopy.

Journal: BMC research notes 20120101

Title: The effects of heat shock protein 90 inhibitors on apoptosis and viral replication in primary effusion lymphoma cells.

Journal: Biological & pharmaceutical bulletin 20120101

Title: Effects of Hsp90 inhibitors, geldanamycin and its analog, on ceramide metabolism and cytotoxicity in PC12 cells.

Journal: The Journal of toxicological sciences 20120101

Title: The role of hypoxia inducible factor-1α in the increased MMP-2 and MMP-9 production by human monocytes exposed to nickel nanoparticles.

Journal: Nanotoxicology 20111201

Title: Pharmacological inhibition of HSP90 activity negatively modulates myogenic differentiation and cell survival in C2C12 cells.

Journal: Molecular and cellular biochemistry 20111201

Title: Clusterin is a critical downstream mediator of stress-induced YB-1 transactivation in prostate cancer.

Journal: Molecular cancer research : MCR 20111201

Title: Inhibition of RPE cell sterile inflammatory responses and endotoxin-induced uveitis by a cell-impermeable HSP90 inhibitor.

Journal: Experimental eye research 20111201

Title: Synthesis and evaluation of poly(styrene-co-maleic acid) micellar nanocarriers for the delivery of tanespimycin.

Journal: International journal of pharmaceutics 20111125

Title: Phase I and pharmacological study of cytarabine and tanespimycin in relapsed and refractory acute leukemia.

Journal: Haematologica 20111101

Title: ATP analog enhances the actions of a heat shock protein 90 inhibitor in multiple myeloma cells.

Journal: The Journal of pharmacology and experimental therapeutics 20111101

Title: Identifying inhibitors of epithelial-mesenchymal transition by connectivity map-based systems approach.

Journal: Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20111101

Title: Multi-drug delivery to tumor cells via micellar nanocarriers.

Journal: International journal of pharmaceutics 20111031

Title: Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone.

Journal: Journal of medicinal chemistry 20111027

Title: The heat shock protein 90 inhibitor IPI-504 induces KIT degradation, tumor shrinkage, and cell proliferation arrest in xenograft models of gastrointestinal stromal tumors.

Journal: Molecular cancer therapeutics 20111001

Title: Lead generation of heat shock protein 90 inhibitors by a combination of fragment-based approach, virtual screening, and structure-based drug design.

Journal: Bioorganic & medicinal chemistry letters 20111001

Title: Exploiting cancer cell vulnerabilities to develop a combination therapy for ras-driven tumors.

Journal: Cancer cell 20110913

Title: Novel insights into the role of HSP90 in cytoprotection of H2S against chemical hypoxia-induced injury in H9c2 cardiac myocytes.

Journal: International journal of molecular medicine 20110901

Title: Heat shock protein 90 inhibition results in altered downstream signaling of mutant KIT and exerts synergistic effects on Kasumi-1 cells when combining with histone deacetylase inhibitor.

Journal: Leukemia research 20110901

Title: Clusterin inhibition using OGX-011 synergistically enhances Hsp90 inhibitor activity by suppressing the heat shock response in castrate-resistant prostate cancer.

Journal: Cancer research 20110901

Title: The Novel HSP90 inhibitor, IPI-493, is highly effective in human gastrostrointestinal stromal tumor xenografts carrying heterogeneous KIT mutations.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20110901

Title: Synthesis and evaluation of biotinylated sansalvamide A analogs and their modulation of Hsp90.

Journal: Bioorganic & medicinal chemistry letters 20110815

Title: HSP90 inhibition is effective in breast cancer: a phase II trial of tanespimycin (17-AAG) plus trastuzumab in patients with HER2-positive metastatic breast cancer progressing on trastuzumab.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20110801

Title: A 3-in-1 polymeric micelle nanocontainer for poorly water-soluble drugs.

Journal: Molecular pharmaceutics 20110801

Title: Why is this effective HSP90 inhibitor not being developed in HER2+ breast cancer?

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20110801

Title: [Development of novel agents for multiple myeloma; now and the future].

Journal: [Rinsho ketsueki] The Japanese journal of clinical hematology 20110801

Title: Impaired infectivity of ritonavir-resistant HIV is rescued by heat shock protein 90AB1.

Journal: The Journal of biological chemistry 20110715

Title: HSP70 inhibition by the small-molecule 2-phenylethynesulfonamide impairs protein clearance pathways in tumor cells.

Journal: Molecular cancer research : MCR 20110701

Title: Chaxamycins A-D, bioactive ansamycins from a hyper-arid desert Streptomyces sp.

Journal: Journal of natural products 20110624

Title: Determination of the volume changes induced by ligand binding to heat shock protein 90 using high-pressure denaturation.

Journal: Analytical biochemistry 20110615

Title: Fibroblast growth factor receptor 3 (FGFR3) is a strong heat shock protein 90 (Hsp90) client: implications for therapeutic manipulation.

Journal: The Journal of biological chemistry 20110603

Title: The Hsp90 inhibitor IPI-504 rapidly lowers EML4-ALK levels and induces tumor regression in ALK-driven NSCLC models.

Journal: Oncogene 20110602

Title: Phase I study of 17-allylamino-17 demethoxygeldanamycin, gemcitabine and/or cisplatin in patients with refractory solid tumors.

Journal: Investigational new drugs 20110601

Title: Hsp90 regulates NADPH oxidase activity and is necessary for superoxide but not hydrogen peroxide production.

Journal: Antioxidants & redox signaling 20110601

Title: Tanespimycin and bortezomib combination treatment in patients with relapsed or relapsed and refractory multiple myeloma: results of a phase 1/2 study.

Journal: British journal of haematology 20110601

Title: Tanespimycin pharmacokinetics: a randomized dose-escalation crossover phase 1 study of two formulations.

Journal: Cancer chemotherapy and pharmacology 20110501

Title: Protection of murine neural progenitor cells by the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin in the low nanomolar concentration range.

Journal: Journal of neurochemistry 20110501

Title: Blockade of Hsp90 by 17AAG antagonizes MDMX and synergizes with Nutlin to induce p53-mediated apoptosis in solid tumors.

Journal: Cell death & disease 20110501

Title: [Effect of heat shock protein 90 inhibitor 17-dimethylamino-ethylaminogeldanamycin on TNfalpha-mediated apoptosis and TNF-induced NF-kappaB activation].

Journal: Sichuan da xue xue bao. Yi xue ban = Journal of Sichuan University. Medical science edition 20110501

Title: Heat shock protein 90-sheltered overexpression of insulin-like growth factor 1 receptor contributes to malignancy of thymic epithelial tumors.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20110415

Title: In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20110401

Title: Synergistic administration of photothermal therapy and chemotherapy to cancer cells using polypeptide-based degradable plasmonic matrices.

Journal: Nanomedicine (London, England) 20110401

Title: A serotype 5/3 adenovirus expressing MDA-7/IL-24 infects renal carcinoma cells and promotes toxicity of agents that increase ROS and ceramide levels.

Journal: Molecular pharmacology 20110301

Title: Role for NAD(P)H:quinone oxidoreductase 1 and manganese-dependent superoxide dismutase in 17-(allylamino)-17-demethoxygeldanamycin-induced heat shock protein 90 inhibition in pancreatic cancer cells.

Journal: The Journal of pharmacology and experimental therapeutics 20110301

Title: HSP90 is crucial for regulation of LAT expression in activated T cells.

Journal: Molecular immunology 20110301

Title: Identification of aneuploidy-selective antiproliferation compounds.

Journal: Cell 20110218

Title: Carbamazepine promotes Her-2 protein degradation in breast cancer cells by modulating HDAC6 activity and acetylation of Hsp90.

Journal: Molecular and cellular biochemistry 20110201

Title: Inhibition of heat shock protein 90 (HSP90) as a therapeutic strategy for the treatment of myeloma and other cancers.

Journal: British journal of haematology 20110201

Title: Tanespimycin as antitumor therapy.

Journal: Clinical lymphoma, myeloma & leukemia 20110201

Title: The role of heat shock protein 90 in the regulation of tumor cell apoptosis.

Journal: Bulletin of experimental biology and medicine 20110201

Title: The Hsp90 inhibitor IPI-504 overcomes bortezomib resistance in mantle cell lymphoma in vitro and in vivo by down-regulation of the prosurvival ER chaperone BiP/Grp78.

Journal: Blood 20110127

Title: 17-AAG increases autophagic removal of mutant androgen receptor in spinal and bulbar muscular atrophy.

Journal: Neurobiology of disease 20110101

Title: Mechanisms by which interleukin-6 regulates prostate-specific antigen gene expression in prostate LNCaP carcinoma cells.

Journal: Journal of andrology 20110101

Title: Targeted inhibition of multiple receptor tyrosine kinases in mesothelioma.

Journal: Neoplasia (New York, N.Y.) 20110101

Title: Expression-based in silico screening of candidate therapeutic compounds for lung adenocarcinoma.

Journal: PloS one 20110101

Title: High-content, high-throughput analysis of cell cycle perturbations induced by the HSP90 inhibitor XL888.

Journal: PloS one 20110101

Title: Cytotoxicity testing: measuring viable cells, dead cells, and detecting mechanism of cell death.

Journal: Methods in molecular biology (Clifton, N.J.) 20110101

Title: SNX-2112, a novel Hsp90 inhibitor, induces G2/M cell cycle arrest and apoptosis in MCF-7 cells.

Journal: Bioscience, biotechnology, and biochemistry 20110101

Title: Sulforaphane potentiates the efficacy of 17-allylamino 17-demethoxygeldanamycin against pancreatic cancer through enhanced abrogation of Hsp90 chaperone function.

Journal: Nutrition and cancer 20110101

Title: [Heat shock protein 90--modulator of TNFalpha-induced apoptosis of Jurkat tumor cells].

Journal: Vestnik Rossiiskoi akademii meditsinskikh nauk 20110101

Title: Targeting HSP90 in ovarian cancers with multiple receptor tyrosine kinase coactivation.

Journal: Molecular cancer 20110101

Title: Magnetic resonance spectroscopy detectable metabolomic fingerprint of response to antineoplastic treatment.

Journal: PloS one 20110101

Title: Assessment of hypoxia inducible factor levels in cancer cell lines upon hypoxic induction using a novel reporter construct.

Journal: PloS one 20110101

Title: Hsp90 (heat shock protein 90) inhibitor occupancy is a direct determinant of client protein degradation and tumor growth arrest in vivo.

Journal: The Journal of biological chemistry 20101217

Title: N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20101215

Title: Mineralocorticoid receptor degradation is promoted by Hsp90 inhibition and the ubiquitin-protein ligase CHIP.

Journal: American journal of physiology. Renal physiology 20101201

Title: Assaying pharmacodynamic endpoints with targeted therapy: flavopiridol and 17AAG induced dephosphorylation of histone H1.5 in acute myeloid leukemia.

Journal: Proteomics 20101201

Title: Heat shock protein 90 regulates the expression of Wilms tumor 1 protein in myeloid leukemias.

Journal: Blood 20101125

Title: Activity of IPI-504, a novel heat-shock protein 90 inhibitor, in patients with molecularly defined non-small-cell lung cancer.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20101120

Title: Prevention of autosomal dominant retinitis pigmentosa by systemic drug therapy targeting heat shock protein 90 (Hsp90).

Journal: Human molecular genetics 20101115

Title: Schwann cell autophagy induced by SAHA, 17-AAG, or clonazepam can reduce bortezomib-induced peripheral neuropathy.

Journal: British journal of cancer 20101109

Title: Identification of a novel HSP70-binding cochaperone critical to HSP90-mediated activation of small serine/threonine kinase.

Journal: The Journal of biological chemistry 20101105

Title: Heat shock protein 90 inhibition depletes LATS1 and LATS2, two regulators of the mammalian hippo tumor suppressor pathway.

Journal: Cancer research 20101101

Title: Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.

Journal: Bioorganic & medicinal chemistry letters 20101101

Title: Targeting heat shock protein 72 enhances Hsp90 inhibitor-induced apoptosis in myeloma.

Journal: Leukemia 20101001

Title: The novel Hsp-90 inhibitor SNX7081 is significantly more potent than 17-AAG against primary CLL cells and a range of haematological cell lines, irrespective of lesions in the TP53 pathway.

Journal: British journal of haematology 20101001

Title: Protection of oligodendrocyte precursor cells by low doses of HSP90 inhibitors in cell culture.

Journal: Experimental neurology 20100901

Title: Molecular markers for novel therapies in neuroendocrine (carcinoid) tumors.

Journal: Endocrine-related cancer 20100901

Title: Inhibition of heat-shock protein 90 reduces Ebola virus replication.

Journal: Antiviral research 20100801

Title: Geldanamycin and its analog induce cytotoxicity in cultured human retinal pigment epithelial cells.

Journal: Experimental eye research 20100801

Title: Tanespimycin monotherapy in relapsed multiple myeloma: results of a phase 1 dose-escalation study.

Journal: British journal of haematology 20100801

Title: Tanespimycin with bortezomib: activity in relapsed/refractory patients with multiple myeloma.

Journal: British journal of haematology 20100801

Title: Safety, efficacy, pharmacokinetics, and pharmacodynamics of the combination of sorafenib and tanespimycin.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20100715

Title: RET is a heat shock protein 90 (HSP90) client protein and is knocked down upon HSP90 pharmacological block.

Journal: The Journal of clinical endocrinology and metabolism 20100701

Title: Modulation of melanoma cell phospholipid metabolism in response to heat shock protein 90 inhibition.

Journal: Oncotarget 20100701

Title: Phosphatidylcholine metabolic transformation and progression signature as a pharmacodynamic biomarker.

Journal: Oncotarget 20100701

Title: A simple yeast-based system for analyzing inhibitor resistance in the human cancer drug targets Hsp90alpha/beta.

Journal: Biochemical pharmacology 20100601

Title: Reactive oxygen species mediate hepatotoxicity induced by the Hsp90 inhibitor geldanamycin and its analogs.

Journal: Free radical biology & medicine 20100601

Title: HSP90 inhibitors induce desensitization of EGF receptor via p38 MAPK-mediated phosphorylation at Ser1046/1047 in human pancreatic cancer cells.

Journal: Oncology reports 20100601

Title: Heat shock protein 90 inhibitors attenuate inflammatory responses in atherosclerosis.

Journal: Cardiovascular research 20100501

Title: Hsp90 inhibitors: a potential treatment for latent EBV infection?

Journal: Cell cycle (Georgetown, Tex.) 20100501

Title: 17-allylamino-17-demethoxygeldanamycin and MEK1/2 inhibitors kill GI tumor cells via Ca2+-dependent suppression of GRP78/BiP and induction of ceramide and reactive oxygen species.

Journal: Molecular cancer therapeutics 20100501

Title: Specific regulation of noncanonical p38alpha activation by Hsp90-Cdc37 chaperone complex in cardiomyocyte.

Journal: Circulation research 20100430

Title: Hsp90 directly modulates the spatial distribution of AF9/MLLT3 and affects target gene expression.

Journal: The Journal of biological chemistry 20100416

Title: Targeting the 90 kDa heat shock protein improves photodynamic therapy.

Journal: Cancer letters 20100328

Title: Combination therapy for hepatitis C virus with heat-shock protein 90 inhibitor 17-AAG and proteasome inhibitor MG132.

Journal: Antiviral chemistry & chemotherapy 20100309

Title: 17-AAG, a Hsp90 inhibitor, attenuates the hypoxia-induced expression of SDF-1alpha and ILK in mouse RPE cells.

Journal: Molecular biology reports 20100301

Title: BIIB021, a novel Hsp90 inhibitor, sensitizes head and neck squamous cell carcinoma to radiotherapy.

Journal: International journal of cancer 20100301

Title: BIIB021, a synthetic Hsp90 inhibitor, has broad application against tumors with acquired multidrug resistance.

Journal: International journal of cancer 20100301

Title: [Management of metastatic HER2-positive breast cancer: present and future].

Journal: Bulletin du cancer 20100301

Title: Hsp90-functionalized polypyrrole nanotube FET sensor for anti-cancer agent detection.

Journal: Biosensors & bioelectronics 20100215

Title: Heat shock protein 90: inhibitors in clinical trials.

Journal: Journal of medicinal chemistry 20100114

Title: The Hsp90 cochaperone, FKBP51, increases Tau stability and polymerizes microtubules.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20100113

Title: Inhibition of 90-kD heat shock protein potentiates the cytotoxicity of chemotherapeutic agents in human glioma cells.

Journal: Journal of neurosurgery 20100101

Title: 17-AAG induces cytoplasmic alpha-synuclein aggregate clearance by induction of autophagy.

Journal: PloS one 20100101

Title: Targeting Hsp90 with small molecule inhibitors induces the over-expression of the anti-apoptotic molecule, survivin, in human A549, HONE-1 and HT-29 cancer cells.

Journal: Molecular cancer 20100101

Title: Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin inhibits the proliferation of ARPE-19 cells.

Journal: Journal of biomedical science 20100101

Title: Bcl-2 regulates HIF-1alpha protein stabilization in hypoxic melanoma cells via the molecular chaperone HSP90.

Journal: PloS one 20100101

Title: 17-Allylamino-17-demethoxygeldanamycin induces downregulation of critical Hsp90 protein clients and results in cell cycle arrest and apoptosis of human urinary bladder cancer cells.

Journal: BMC cancer 20100101

Title: Molecular signature of response and potential pathways related to resistance to the HSP90 inhibitor, 17AAG, in breast cancer.

Journal: BMC medical genomics 20100101

Title: 17-allyamino-17-demethoxygeldanamycin treatment results in a magnetic resonance spectroscopy-detectable elevation in choline-containing metabolites associated with increased expression of choline transporter SLC44A1 and phospholipase A2.

Journal: Breast cancer research : BCR 20100101

Title: The antiproliferative activity of the heat shock protein 90 inhibitor IPI-504 is not dependent on NAD(P)H:quinone oxidoreductase 1 activity in vivo.

Journal: Molecular cancer therapeutics 20091201

Title: Induction of E-cadherin in lung cancer and interaction with growth suppression by histone deacetylase inhibition.

Journal: Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20091201

Title: Inhibition of constitutive and cxc-chemokine-induced NF-kappaB activity potentiates ansamycin-based HSP90-inhibitor cytotoxicity in castrate-resistant prostate cancer cells.

Journal: British journal of cancer 20091103

Title: Proton MRS detects metabolic changes in hormone sensitive and resistant human prostate cancer models CWR22 and CWR22r.

Journal: Magnetic resonance in medicine 20091101

Title: [Molecular therapy targeting protein misfolding and aggregation for the polyglutamine diseases].

Journal: Rinsho shinkeigaku = Clinical neurology 20091101

Title: Anti-proliferative activity of heat shock protein (Hsp) 90 inhibitors via beta-catenin/TCF7L2 pathway in adult T cell leukemia cells.

Journal: Cancer letters 20091018

Title: Heat shock protein-90 inhibitors increase MHC class I-related chain A and B ligand expression on multiple myeloma cells and their ability to trigger NK cell degranulation.

Journal: Journal of immunology (Baltimore, Md. : 1950) 20091001

Title: Retaspimycin hydrochloride (IPI-504): a novel heat shock protein inhibitor as an anticancer agent.

Journal: Expert opinion on investigational drugs 20090901

Title: Met amplification and HSP90 inhibitors.

Journal: Cell cycle (Georgetown, Tex.) 20090901

Title: Candidate therapeutic agents for hepatocellular cancer can be identified from phenotype-associated gene expression signatures.

Journal: Cancer 20090815

Title: Enhanced radiosensitization of human glioma cells by combining inhibition of poly(ADP-ribose) polymerase with inhibition of heat shock protein 90.

Journal: Molecular cancer therapeutics 20090801

Title: Antitumor efficacy of IPI-504, a selective heat shock protein 90 inhibitor against human epidermal growth factor receptor 2-positive human xenograft models as a single agent and in combination with trastuzumab or lapatinib.

Journal: Molecular cancer therapeutics 20090801

Title: Three-kinase inhibitor combination recreates multipathway effects of a geldanamycin analogue on hepatocellular carcinoma cell death.

Journal: Molecular cancer therapeutics 20090801

Title: Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.

Journal: Journal of medicinal chemistry 20090723

Title: Hsp90 inhibitors, GA and 17AAG, lead to ER stress-induced apoptosis in rat histiocytoma.

Journal: Biochemical pharmacology 20090715

Title: Zebularine suppresses the apoptotic potential of 5-fluorouracil via cAMP/PKA/CREB pathway against human oral squamous cell carcinoma cells.

Journal: Cancer chemotherapy and pharmacology 20090701

Title: Heat shock protein 90 inhibitor induces apoptosis and attenuates activation of hepatic stellate cells.

Journal: The Journal of pharmacology and experimental therapeutics 20090701

Title: Cancer cells harboring MET gene amplification activate alternative signaling pathways to escape MET inhibition but remain sensitive to Hsp90 inhibitors.

Journal: Cell cycle (Georgetown, Tex.) 20090701

Title: Potent triazolothione inhibitor of heat-shock protein-90.

Journal: Chemical biology & drug design 20090701

Title: Tanespimycin: the opportunities and challenges of targeting heat shock protein 90.

Journal: Expert opinion on investigational drugs 20090601

Title: Heat-shock protein 90 (Hsp90) as a molecular target for therapy of gastrointestinal cancer.

Journal: Anticancer research 20090601

Title: Potent cytotoxic C-11 modified geldanamycin analogues.

Journal: Journal of medicinal chemistry 20090528

Title: Transcription inhibition of heat shock proteins: a strategy for combination of 17-allylamino-17-demethoxygeldanamycin and actinomycin d.

Journal: Cancer research 20090501

Title: Integration of ligand and structure-based virtual screening for the identification of the first dual targeting agent for heat shock protein 90 (Hsp90) and tubulin.

Journal: Journal of medicinal chemistry 20090423

Title: Gene expression patterns in mismatch repair-deficient colorectal cancers highlight the potential therapeutic role of inhibitors of the phosphatidylinositol 3-kinase-AKT-mammalian target of rapamycin pathway.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20090415

Title: Efficacy of the HSP90 inhibitor 17-AAG in human glioma cell lines and tumorigenic glioma stem cells.

Journal: Neuro-oncology 20090401

Title: A cremophor-free formulation for tanespimycin (17-AAG) using PEO-b-PDLLA micelles: characterization and pharmacokinetics in rats.

Journal: Journal of pharmaceutical sciences 20090401

Title: High cytotoxic sensitivity of the oligodendrocyte precursor cells to HSP90 inhibitors in cell cultures.

Journal: Experimental neurology 20090401

Title: Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.

Journal: Journal of medicinal chemistry 20090326

Title: Discovery and development of heat shock protein 90 inhibitors.

Journal: Bioorganic & medicinal chemistry 20090315

Title: Acquired resistance to 17-allylamino-17-demethoxygeldanamycin (17-AAG, tanespimycin) in glioblastoma cells.

Journal: Cancer research 20090301

Title: The heat shock protein 90 inhibitor IPI-504 induces apoptosis of AKT-dependent diffuse large B-cell lymphomas.

Journal: British journal of haematology 20090201

Title: Targeted therapy of human osteosarcoma with 17AAG or rapamycin: characterization of induced apoptosis and inhibition of mTOR and Akt/MAPK/Wnt pathways.

Journal: International journal of oncology 20090201

Title: An experimental study on the antitumor effect of 131I-17-AAG in vitro and in vivo.

Journal: Annals of nuclear medicine 20090201

Title: Hsp90 is expressed and represents a therapeutic target in human oesophageal cancer using the inhibitor 17-allylamino-17-demethoxygeldanamycin.

Journal: British journal of cancer 20090127

Title: VIP-grafted sterically stabilized phospholipid nanomicellar 17-allylamino-17-demethoxy geldanamycin: a novel targeted nanomedicine for breast cancer.

Journal: International journal of pharmaceutics 20090105

Title: 90-kDa heat shock protein inhibition abrogates the topoisomerase I poison-induced G2/M checkpoint in p53-null tumor cells by depleting Chk1 and Wee1.

Journal: Molecular pharmacology 20090101

Title: Effectiveness of 17DMAG, a geldanamycin derivative, in murine acute myeloid leukemia.

Journal: Acta haematologica 20090101

Title: COMMD1 Promotes pVHL and O2-Independent Proteolysis of HIF-1alpha via HSP90/70.

Journal: PloS one 20090101

Title: Inhibition and function of heat shock proteins 70 and 90.

Journal: Current topics in medicinal chemistry 20090101

Title: Stability of the Hsp90 inhibitor 17AAG hydroquinone and prevention of metal-catalyzed oxidation.

Journal: Journal of pharmaceutical sciences 20081201

Title: Expression of interleukin-6 is downregulated by 17-(allylamino)-17-demethoxygeldanamycin in human prostatic carcinoma cells.

Journal: Acta pharmacologica Sinica 20081101

Title: Heat shock protein 90 inhibitors suppress aryl hydrocarbon receptor-mediated activation of CYP1A1 and CYP1B1 transcription and DNA adduct formation.

Journal: Cancer prevention research (Philadelphia, Pa.) 20081101

Title: A phase 1 dose-escalation study of irinotecan in combination with 17-allylamino-17-demethoxygeldanamycin in patients with solid tumors.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20081015

Title: An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models.

Journal: Cancer chemotherapy and pharmacology 20081001

Title: Molecular and biologic characterization and drug sensitivity of pan-histone deacetylase inhibitor-resistant acute myeloid leukemia cells.

Journal: Blood 20081001

Title: Optimizing natural products by biosynthetic engineering: discovery of nonquinone Hsp90 inhibitors.

Journal: Journal of medicinal chemistry 20080925

Title: Targeting Hsp90 prevents escape of breast cancer cells from tyrosine kinase inhibition.

Journal: Cell cycle (Georgetown, Tex.) 20080915

Title: Activity of dasatinib, a dual SRC/ABL kinase inhibitor, and IPI-504, a heat shock protein 90 inhibitor, against gastrointestinal stromal tumor-associated PDGFRAD842V mutation.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20080915

Title: P-Glycoprotein-mediated resistance to Hsp90-directed therapy is eclipsed by the heat shock response.

Journal: Cancer research 20080915

Title: Dual targeting of HSC70 and HSP72 inhibits HSP90 function and induces tumor-specific apoptosis.

Journal: Cancer cell 20080909

Title: The heat shock protein antagonist 17-AAG potentiates the activity of enzastaurin against malignant human glioma cells.

Journal: Cancer letters 20080908

Title: HDAC6 inhibition enhances 17-AAG--mediated abrogation of hsp90 chaperone function in human leukemia cells.

Journal: Blood 20080901

Title: Mitogen-activated protein kinase kinase 1/2 inhibitors and 17-allylamino-17-demethoxygeldanamycin synergize to kill human gastrointestinal tumor cells in vitro via suppression of c-FLIP-s levels and activation of CD95.

Journal: Molecular cancer therapeutics 20080901

Title: Heat shock protein 90-binding agents protect renal cells from oxidative stress and reduce kidney ischemia-reperfusion injury.

Journal: American journal of physiology. Renal physiology 20080801

Title: Combination of rapamycin and 17-allylamino-17-demethoxygeldanamycin abrogates Akt activation and potentiates mTOR blockade in breast cancer cells.

Journal: Anti-cancer drugs 20080801

Title: Development and validation of a rapid and sensitive high-performance liquid chromatography-mass spectroscopy assay for determination of 17-(allylamino)-17-demethoxygeldanamycin and 17-(amino)-17-demethoxygeldanamycin in human plasma.

Journal: Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20080801

Title: Radiosensitization of human vascular endothelial cells through Hsp90 inhibition with 17-N-allilamino-17-demethoxygeldanamycin.

Journal: International journal of radiation oncology, biology, physics 20080701

Title: Role of acetylation and extracellular location of heat shock protein 90alpha in tumor cell invasion.

Journal: Cancer research 20080615

Title: 17-AAG and 17-DMAG-induced inhibition of cell proliferation through B-Raf downregulation in WT B-Raf-expressing uveal melanoma cell lines.

Journal: Investigative ophthalmology & visual science 20080601

Title: RNAi-mediated silencing of p190Bcr-Abl inactivates Stat5 and cooperates with imatinib mesylate and 17-allylamino-17-demetoxygeldanamycin in selective killing of p190Bcr-Abl-expressing leukemia cells.

Journal: Leukemia 20080601

Title: Resveratrol induces apoptosis in K562 (chronic myelogenous leukemia) cells by targeting a key survival protein, heat shock protein 70.

Journal: Cancer science 20080601

Title: Arsenic trioxide decreases AKT protein in a caspase-dependent manner.

Journal: Molecular cancer therapeutics 20080601

Title: Chaperone-dependent stabilization and degradation of p53 mutants.

Journal: Oncogene 20080529

Title: IPI-504, a novel and soluble HSP-90 inhibitor, blocks the unfolded protein response in multiple myeloma cells.

Journal: Cancer chemotherapy and pharmacology 20080501

Title: Dopamine-induced toxicity is synergistically potentiated by simultaneous HSP-90 and Akt inhibition in oligodendrocyte progenitors.

Journal: Journal of neurochemistry 20080501

Title: Heat shock protein 90 inhibition is cytotoxic to primary AML cells expressing mutant FLT3 and results in altered downstream signalling.

Journal: British journal of haematology 20080501

Title: Geldanamycin enhances hepatocyte growth factor stimulation of eNOS phosphorylation in endothelial cells.

Journal: European journal of pharmacology 20080317

Title: Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity.

Journal: Bioorganic & medicinal chemistry letters 20080301

Title: Prevention of chemotherapy-induced alopecia in rodent models.

Journal: Cell stress & chaperones 20080301

Title: 4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.

Journal: Journal of medicinal chemistry 20080124

Title: Inhibition of Hsp90 down-regulates mutant epidermal growth factor receptor (EGFR) expression and sensitizes EGFR mutant tumors to paclitaxel.

Journal: Cancer research 20080115

Title: Divergent synthesis of a pochonin library targeting HSP90 and in vivo efficacy of an identified inhibitor.

Journal: Angewandte Chemie (International ed. in English) 20080101

Title: Heat shock protein-90-alpha, a prolactin-STAT5 target gene identified in breast cancer cells, is involved in apoptosis regulation.

Journal: Breast cancer research : BCR 20080101

Title: A highly invasive human glioblastoma pre-clinical model for testing therapeutics.

Journal: Journal of translational medicine 20080101

Title: Cystine-glutamate transporter SLC7A11 mediates resistance to geldanamycin but not to 17-(allylamino)-17-demethoxygeldanamycin.

Journal: Molecular pharmacology 20071201

Title: Rituximab and 17-allylamino-17-demethoxygeldanamycin induce synergistic apoptosis in B-cell chronic lymphocytic leukaemia.

Journal: British journal of haematology 20071201

Title: Combination of trastuzumab and tanespimycin (17-AAG, KOS-953) is safe and active in trastuzumab-refractory HER-2 overexpressing breast cancer: a phase I dose-escalation study.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20071201

Title: SEPT9_V1 protein expression is associated with human cancer cell resistance to microtubule-disrupting agents.

Journal: Cancer biology & therapy 20071201

Title: Targeting heat shock protein 90 in pancreatic cancer impairs insulin-like growth factor-I receptor signaling, disrupts an interleukin-6/signal-transducer and activator of transcription 3/hypoxia-inducible factor-1alpha autocrine loop, and reduces orthotopic tumor growth.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20071101

Title: Heat shock protein 90 inhibitors prolong survival, attenuate inflammation, and reduce lung injury in murine sepsis.

Journal: American journal of respiratory and critical care medicine 20071001

Title: Intratumor injection of the Hsp90 inhibitor 17AAG decreases tumor growth and induces apoptosis in a prostate cancer xenograft model.

Journal: The Journal of urology 20071001

Title: The heat-shock protein 90 inhibitor, geldanamycin, induces apoptotic cell death in Epstein-Barr virus-positive NK/T-cell lymphoma by Akt down-regulation.

Journal: The Journal of pathology 20071001

Title: Apoptosis-based dual molecular targeting by INNO-406, a second-generation Bcr-Abl inhibitor, and ABT-737, an inhibitor of antiapoptotic Bcl-2 proteins, against Bcr-Abl-positive leukemia.

Journal: Cell death and differentiation 20070901

Title: The geldanamycin analogue 17-allylamino-17-demethoxygeldanamycin inhibits the growth of GL261 glioma cells in vitro and in vivo.

Journal: Anti-cancer drugs 20070901

Title: Inhibition of Hsp90 attenuates inflammation in endotoxin-induced uveitis.

Journal: FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20070701

Title: Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity.

Journal: Journal of medicinal chemistry 20070614

Title: Geldanamycin derivatives and neuroprotective effect on cultured P19-derived neurons.

Journal: Bioorganic & medicinal chemistry letters 20070515

Title: Survivin, a member of the inhibitor of apoptosis family, is induced by photodynamic therapy and is a target for improving treatment response.

Journal: Cancer research 20070515

Title: Regulation of death-associated protein kinase. Stabilization by HSP90 heterocomplexes.

Journal: The Journal of biological chemistry 20070420

Title: Inhibition of heat shock protein-90 modulates multiple functions required for survival of human T-cell leukemia virus type I-infected T-cell lines and adult T-cell leukemia cells.

Journal: International journal of cancer 20070415

Title: Proteomic analysis of waldenstrom macroglobulinemia.

Journal: Cancer research 20070415

Title: Evaluation of plasma insulin-like growth factor binding protein 2 and Her-2 extracellular domain as biomarkers for 17-allylamino-17-demethoxygeldanamycin treatment of adult patients with advanced solid tumors.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20070401

Title: Synergism between arsenic trioxide and heat shock protein 90 inhibitors on signal transducer and activator of transcription protein 3 activity--pharmacodynamic drug-drug interaction modeling.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20070401

Title: Gene and protein expression profiling of human ovarian cancer cells treated with the heat shock protein 90 inhibitor 17-allylamino-17-demethoxygeldanamycin.

Journal: Cancer research 20070401

Title: Phase I pharmacokinetic and pharmacodynamic study of 17-N-allylamino-17-demethoxygeldanamycin in pediatric patients with recurrent or refractory solid tumors: a pediatric oncology experimental therapeutics investigators consortium study.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20070315

Title: Different target range and cytotoxic specificity of adaphostin and 17-allylamino-17-demethoxygeldanamycin in imatinib-resistant and sensitive cell lines.

Journal: Leukemia 20070301

Title: Synergism between etoposide and 17-AAG in leukemia cells: critical roles for Hsp90, FLT3, topoisomerase II, Chk1, and Rad51.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20070301

Title: Inhibition of heat shock protein 90 impairs epidermal growth factor-mediated signaling in gastric cancer cells and reduces tumor growth and vascularization in vivo.

Journal: Molecular cancer therapeutics 20070301

Title: Multiple myeloma therapies.

Journal: Nature reviews. Drug discovery 20070301

Title: Dimeric ansamycins--a new class of antitumor Hsp90 modulators with prolonged inhibitory activity.

Journal: International journal of cancer 20070215

Title: Heat shock protein 90 and ErbB2 in the cardiac response to doxorubicin injury.

Journal: Cancer research 20070215

Title: Geldanamycin treatment reduces neovascularization in a mouse model of retinopathy of prematurity.

Journal: Graefe's archive for clinical and experimental ophthalmology = Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie 20070201

Title: BIRB 796 enhances cytotoxicity triggered by bortezomib, heat shock protein (Hsp) 90 inhibitor, and dexamethasone via inhibition of p38 mitogen-activated protein kinase/Hsp27 pathway in multiple myeloma cell lines and inhibits paracrine tumour growth.

Journal: British journal of haematology 20070201

Title: American Society of Hematology--48th Annual Meeting and Exposition. Updates on hematological therapies. 9-12 December 2006 Orlando, FL, USA.

Journal: IDrugs : the investigational drugs journal 20070201

Title: 17-Allylamino-17-demethoxygeldanamycin enhances the lethality of deoxycholic acid in primary rodent hepatocytes and established cell lines.

Journal: Molecular cancer therapeutics 20070201

Title: [Integrated molecular medicine for neuronal and neoplastic disorders].

Journal: Seikagaku. The Journal of Japanese Biochemical Society 20070201

Title: RACK1 competes with HSP90 for binding to HIF-1alpha and is required for O(2)-independent and HSP90 inhibitor-induced degradation of HIF-1alpha.

Journal: Molecular cell 20070126

Title: Evolutionary constraints on chaperone-mediated folding provide an antiviral approach refractory to development of drug resistance.

Journal: Genes & development 20070115

Title: The platelet-derived growth factor receptor alpha is destabilized by geldanamycins in cancer cells.

Journal: The Journal of biological chemistry 20070105

Title: Biotransformation of geldanamycin and 17-allylamino-17-demethoxygeldanamycin by human liver microsomes: reductive versus oxidative metabolism and implications.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20070101

Title: Small molecule inducers of heat-shock response reduce polyQ-mediated huntingtin aggregation. A possible therapeutic strategy.

Journal: Neuro-degenerative diseases 20070101

Title: Development of new mouse lung tumor models expressing EGFR T790M mutants associated with clinical resistance to kinase inhibitors.

Journal: PloS one 20070101

Title: Mechanisms of Legionella pneumophila-induced interleukin-8 expression in human lung epithelial cells.

Journal: BMC microbiology 20070101

Title: Drug-mediated targeted disruption of multiple protein activities through functional inhibition of the Hsp90 chaperone complex.

Journal: Current medicinal chemistry 20070101

Title: Small-molecule targeting of heat shock protein 90 chaperone function: rational identification of a new anticancer lead.

Journal: Journal of medicinal chemistry 20061228

Title: The heat-shock protein 90 inhibitor 17-allylamino-17-demethoxygeldanamycin suppresses glial inflammatory responses and ameliorates experimental autoimmune encephalomyelitis.

Journal: Journal of neurochemistry 20061201

Title: The HSP90 inhibitor 17-AAG synergizes with doxorubicin and U0126 in anaplastic large cell lymphoma irrespective of ALK expression.

Journal: Experimental hematology 20061201

Title: Targeting of multiple signalling pathways by heat shock protein 90 molecular chaperone inhibitors.

Journal: Endocrine-related cancer 20061201

Title: Up-regulation of heat shock protein 27 induces resistance to 17-allylamino-demethoxygeldanamycin through a glutathione-mediated mechanism.

Journal: Cancer research 20061115

Title: Combination mammalian target of rapamycin inhibitor rapamycin and HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin has synergistic activity in multiple myeloma.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20061115

Title: Induction of multiple heat shock proteins and neuroprotection in a primary culture model of familial amyotrophic lateral sclerosis.

Journal: Neurobiology of disease 20061101

Title: MUC1 oncoprotein functions in activation of fibroblast growth factor receptor signaling.

Journal: Molecular cancer research : MCR 20061101

Title: Heat shock protein 90 inhibition in imatinib-resistant gastrointestinal stromal tumor.

Journal: Cancer research 20060915

Title: Pharmacological induction of Hsp70 protects apoptosis-prone cells from doxorubicin: comparison with caspase-inhibitor- and cycle-arrest-mediated cytoprotection.

Journal: Cell death and differentiation 20060901

Title: Synthesis of a red-shifted fluorescence polarization probe for Hsp90.

Journal: Bioorganic & medicinal chemistry letters 20060901

Title: Modulation of Hsp90 function in neurodegenerative disorders: a molecular-targeted therapy against disease-causing protein.

Journal: Journal of molecular medicine (Berlin, Germany) 20060801

Title: Current and future management of GIST.

Journal: Clinical advances in hematology & oncology : H&O 20060801

Title: Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.

Journal: Journal of medicinal chemistry 20060727

Title: 17-AAG, an Hsp90 inhibitor, causes kinetochore defects: a novel mechanism by which 17-AAG inhibits cell proliferation.

Journal: Oncogene 20060713

Title: Synthesis of Hsp90 dimerization modulators.

Journal: Bioorganic & medicinal chemistry letters 20060701

Title: Analysis of expression of heat shock protein-90 (HSP90) and the effects of HSP90 inhibitor (17-AAG) in multiple myeloma.

Journal: Leukemia & lymphoma 20060701

Title: [Enhancement of HER-2 degradation by carbamazepine in breast cancer SKBR-3 cell line].

Journal: Zhonghua zhong liu za zhi [Chinese journal of oncology] 20060701

Title: The topoisomerase II-Hsp90 complex: a new chemotherapeutic target?

Journal: International journal of cancer 20060601

Title: Treatment with drugs able to reduce iodine efflux significantly increases the intracellular retention time in thyroid cancer cells stably transfected with sodium iodide symporter complementary deoxyribonucleic acid.

Journal: The Journal of clinical endocrinology and metabolism 20060601

Title: Dihydroquinone ansamycins: toward resolving the conflict between low in vitro affinity and high cellular potency of geldanamycin derivatives.

Journal: Biochemistry 20060502

Title: The Hsp90 inhibitor 17-allylamide-17-demethoxygeldanamycin induces apoptosis and differentiation of Kasumi-1 harboring the Asn822Lys KIT mutation and down-regulates KIT protein level.

Journal: Leukemia research 20060501

Title: 4-Amino derivatives of the Hsp90 inhibitor CCT018159.

Journal: Bioorganic & medicinal chemistry letters 20060501

Title: Cooperative inhibitory effect of ZD1839 (Iressa) in combination with 17-AAG on glioma cell growth.

Journal: Molecular carcinogenesis 20060501

Title: Early tumor response to Hsp90 therapy using HER2 PET: comparison with 18F-FDG PET.

Journal: Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20060501

Title: Potentiation of paclitaxel activity by the HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin in human ovarian carcinoma cell lines with high levels of activated AKT.

Journal: Molecular cancer therapeutics 20060501

Title: Identification of new biomarkers for clinical trials of Hsp90 inhibitors.

Journal: Molecular cancer therapeutics 20060501

Title: Identification of genes involved in the sensitivity to antitumour drug 17-allylamino,17-demethoxygeldanamycin (17AAG).

Journal: Molecular bioSystems 20060501

Title: Hsp90 inhibitor 17-AAG reduces ErbB2 levels and inhibits proliferation of the trastuzumab resistant breast tumor cell line JIMT-1.

Journal: Immunology letters 20060415

Title: Heat shock protein 70 neutralization exerts potent antitumor effects in animal models of colon cancer and melanoma.

Journal: Cancer research 20060415

Title: Targeting Hsp90 by 17-AAG in leukemia cells: mechanisms for synergistic and antagonistic drug combinations with arsenic trioxide and Ara-C.

Journal: Leukemia 20060401

Title: Synergistic interactions between DMAG and mitogen-activated protein kinase kinase 1/2 inhibitors in Bcr/abl+ leukemia cells sensitive and resistant to imatinib mesylate.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20060401

Title: Hsp90 inhibitors cause G2/M arrest associated with the reduction of Cdc25C and Cdc2 in lung cancer cell lines.

Journal: Journal of cancer research and clinical oncology 20060301

Title: Benzoquinone ansamycin heat shock protein 90 inhibitors modulate multiple functions required for tumor angiogenesis.

Journal: Molecular cancer therapeutics 20060301

Title: Antimyeloma activity of heat shock protein-90 inhibition.

Journal: Blood 20060201

Title: Heat shock protein 90 is an essential molecular chaperone for nuclear transport of glucocorticoid receptor beta.

Journal: Investigative ophthalmology & visual science 20060201

Title: 17-allylamino-17-demethoxygeldanamycin synergistically potentiates tumor necrosis factor-induced lung cancer cell death by blocking the nuclear factor-kappaB pathway.

Journal: Cancer research 20060115

Title: Inhibition of heat shock protein 90 function by 17-allylamino-17-demethoxy-geldanamycin in Hodgkin's lymphoma cells down-regulates Akt kinase, dephosphorylates extracellular signal-regulated kinase, and induces cell cycle arrest and cell death.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20060115

Title: Synergistic interaction between 17-AAG and phosphatidylinositol 3-kinase inhibition in human malignant glioma cells.

Journal: Molecular carcinogenesis 20060101

Title: Silencing of survivin gene by small interfering RNAs produces supra-additive growth suppression in combination with 17-allylamino-17-demethoxygeldanamycin in human prostate cancer cells.

Journal: Molecular cancer therapeutics 20060101

Title: Hsp90 inhibitors in the clinic.

Journal: Handbook of experimental pharmacology 20060101

Title: Stimulation of proteasome activity as a therapeutic target in schizophrenia: possible usefulness of 17-allylamino-demethoxygeldanamycin.

Journal: Medical hypotheses 20060101

Title: Effect of the Hsp90 modulators on the heat-shock response in eukaryotic cells.

Journal: Folia microbiologica 20060101

Title: Inhibition of neuroblastoma xenograft growth by Hsp90 inhibitors.

Journal: Anticancer research 20060101

Title: In vitro combined modality treatment of prostate carcinoma cells with 17-(allylamino)-17-demethoxygeldanamycin and ionizing radiation.

Journal: Anticancer research 20060101

Title: Inhibitors of the HSP90 molecular chaperone: current status.

Journal: Advances in cancer research 20060101

Title: In vitro detection of differential and cell-specific hepatobiliary toxicity induced by geldanamycin and 17-allylaminogeldanamycin in rats.

Journal: Toxicology in vitro : an international journal published in association with BIBRA 20051201

Title: Structure-based discovery of a new class of Hsp90 inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20051201

Title: 17-AAG: mechanisms of antitumour activity.

Journal: Expert opinion on investigational drugs 20051201

Title: Activated B-RAF is an Hsp90 client protein that is targeted by the anticancer drug 17-allylamino-17-demethoxygeldanamycin.

Journal: Cancer research 20051201

Title: Induction of the hypoxia-inducible factor system by low levels of heat shock protein 90 inhibitors.

Journal: Cancer research 20051201

Title: Heat shock protein 90 inhibitor 17-allylamino-17-demethoxygeldanamycin potentiates the radiation response of tumor cells grown as monolayer cultures and spheroids by inducing apoptosis.

Journal: Cancer science 20051201

Title: Abrogation of heat shock protein 70 induction as a strategy to increase antileukemia activity of heat shock protein 90 inhibitor 17-allylamino-demethoxy geldanamycin.

Journal: Cancer research 20051115

Title: Formation of 17-allylamino-demethoxygeldanamycin (17-AAG) hydroquinone by NAD(P)H:quinone oxidoreductase 1: role of 17-AAG hydroquinone in heat shock protein 90 inhibition.

Journal: Cancer research 20051101

Title: ZAP-70 is a novel conditional heat shock protein 90 (Hsp90) client: inhibition of Hsp90 leads to ZAP-70 degradation, apoptosis, and impaired signaling in chronic lymphocytic leukemia.

Journal: Blood 20051001

Title: In vitro detection of differential and cell-specific hepatobiliary toxicity induced by geldanamycin and 17-allylaminogeldanamycin using dog liver slices.

Journal: Toxicological sciences : an official journal of the Society of Toxicology 20051001

Title: 17-AAG, an Hsp90 inhibitor, ameliorates polyglutamine-mediated motor neuron degeneration.

Journal: Nature medicine 20051001

Title: Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20051001

Title: Targeting toxic proteins for turnover.

Journal: Nature medicine 20051001

Title: Human leukemias with mutated FLT3 kinase are synergistically sensitive to FLT3 and Hsp90 inhibitors: the key role of the STAT5 signal transduction pathway.

Journal: Leukemia 20050901

Title: Chemical ablation of androgen receptor in prostate cancer cells by the histone deacetylase inhibitor LAQ824.

Journal: Molecular cancer therapeutics 20050901

Title: A phase II trial of 17-allylamino-17- demethoxygeldanamycin in patients with hormone-refractory metastatic prostate cancer.

Journal: Clinical prostate cancer 20050901

Title: Geldanamycin derivative inhibition of HGF/SF-mediated Met tyrosine kinase receptor-dependent urokinase-plasminogen activation.

Journal: Bioorganic & medicinal chemistry 20050815

Title: 17-Allylamino-17-demethoxygeldanamycin overcomes TRAIL resistance in colon cancer cell lines.

Journal: Biochemical pharmacology 20050815

Title: Comparison of 17-dimethylaminoethylamino-17-demethoxy-geldanamycin (17DMAG) and 17-allylamino-17-demethoxygeldanamycin (17AAG) in vitro: effects on Hsp90 and client proteins in melanoma models.

Journal: Cancer chemotherapy and pharmacology 20050801

Title: Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin prevents synovial sarcoma proliferation via apoptosis in in vitro models.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20050801

Title: Heat shock protein 90 inhibition sensitizes acute myelogenous leukemia cells to cytarabine.

Journal: Blood 20050701

Title: Lonafarnib reduces the resistance of primitive quiescent CML cells to imatinib mesylate in vitro.

Journal: Leukemia 20050701

Title: Synergistic activity of imatinib and 17-AAG in imatinib-resistant CML cells overexpressing BCR-ABL--Inhibition of P-glycoprotein function by 17-AAG.

Journal: Leukemia 20050701

Title: Heat shock protein 90 indirectly regulates ERK activity by affecting Raf protein metabolism.

Journal: Acta biochimica et biophysica Sinica 20050701

Title: Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.

Journal: Journal of medicinal chemistry 20050630

Title: Phase I pharmacokinetic and pharmacodynamic study of 17-allylamino, 17-demethoxygeldanamycin in patients with advanced malignancies.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20050620

Title: The heat shock protein 90 inhibitor, 17-allylamino-17-demethoxygeldanamycin, enhances osteoclast formation and potentiates bone metastasis of a human breast cancer cell line.

Journal: Cancer research 20050601

Title: Solid-phase immunoassays in mechanism-based drug discovery: their application in the development of inhibitors of the molecular chaperone heat-shock protein 90.

Journal: Assay and drug development technologies 20050601

Title: Heat shock proteins and acute leukemias.

Journal: Hematology (Amsterdam, Netherlands) 20050601

Title: Potent activity of a novel dimeric heat shock protein 90 inhibitor against head and neck squamous cell carcinoma in vitro and in vivo.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20050515

Title: Regulation of glucocorticoid receptor steroid binding and trafficking by the hsp90/hsp70-based chaperone machinery: implications for clinical intervention.

Journal: Leukemia 20050501

Title: Phase I pharmacokinetic-pharmacodynamic study of 17-(allylamino)-17-demethoxygeldanamycin (17AAG, NSC 330507), a novel inhibitor of heat shock protein 90, in patients with refractory advanced cancers.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20050501

Title: Rational design of shepherdin, a novel anticancer agent.

Journal: Cancer cell 20050501

Title: Cotreatment with suberanoylanilide hydroxamic acid and 17-allylamino 17-demethoxygeldanamycin synergistically induces apoptosis in Bcr-Abl+ Cells sensitive and resistant to STI571 (imatinib mesylate) in association with down-regulation of Bcr-Abl, abrogation of signal transducer and activator of transcription 5 activity, and Bax conformational change.

Journal: Molecular pharmacology 20050401

Title: Production of 8-demethylgeldanamycin and 4,5-epoxy-8-demethylgeldanamycin from a recombinant strain of Streptomyces hygroscopicus.

Journal: Journal of natural products 20050401

Title: Heat-shock protein 90 inhibitors in cancer therapy: 17AAG and beyond.

Journal: Future oncology (London, England) 20050401

Title: Phase I and pharmacologic study of 17-(allylamino)-17-demethoxygeldanamycin in adult patients with solid tumors.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20050320

Title: Population pharmacokinetic analysis of 17-(allylamino)-17-demethoxygeldanamycin (17AAG) in adult patients with advanced malignancies.

Journal: Cancer chemotherapy and pharmacology 20050301

Title: Effects of 17-allylamino-17-demethoxygeldanamycin (17-AAG) on pediatric acute lymphoblastic leukemia (ALL) with respect to Bcr-Abl status and imatinib mesylate sensitivity.

Journal: Pediatric research 20050301

Title: The geldanamycin derivative 17-AAG decreases VEGF secretion and leukemia growth support by trisomy 8 myelodysplastic syndrome bone marrow stromal cells.

Journal: Pediatric hematology and oncology 20050301

Title: Phase I trial of 17-allylamino-17-demethoxygeldanamycin in patients with advanced cancer.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20050220

Title: Combination of the histone deacetylase inhibitor LBH589 and the hsp90 inhibitor 17-AAG is highly active against human CML-BC cells and AML cells with activating mutation of FLT-3.

Journal: Blood 20050215

Title: 17-Allyamino-17-demethoxygeldanamycin and 17-NN-dimethyl ethylene diamine-geldanamycin have cytotoxic activity against multiple gynecologic cancer cell types.

Journal: Gynecologic oncology 20050201

Title: Induction of angiogenesis by heat shock protein 90 mediated by protein kinase Akt and endothelial nitric oxide synthase.

Journal: Arteriosclerosis, thrombosis, and vascular biology 20041201

Title: Inhibition of heat shock protein 90, a novel RET/PTC1-associated protein, increases radioiodide accumulation in thyroid cells.

Journal: The Journal of biological chemistry 20041015

Title: Hsp90: an emerging target for breast cancer therapy.

Journal: Anti-cancer drugs 20040801

Title: Altered Hsp90 function in cancer: a unique therapeutic opportunity.

Journal: Molecular cancer therapeutics 20040801

Title: [Heat shock protein 90: novel target for cancer therapy].

Journal: Ai zheng = Aizheng = Chinese journal of cancer 20040801

Title: Antiangiogenic properties of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin: an orally bioavailable heat shock protein 90 modulator.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20040715

Title: Imaging the pharmacodynamics of HER2 degradation in response to Hsp90 inhibitors.

Journal: Nature biotechnology 20040601

Title: An image worth a thousand lives?

Journal: Nature biotechnology 20040601

Title: Therapeutic and diagnostic implications of Hsp90 activation.

Journal: Trends in molecular medicine 20040601

Title: 17-Allylamino-17-demethoxygeldanamycin activity against thyroid cancer cell lines correlates with heat shock protein 90 levels.

Journal: The Journal of clinical endocrinology and metabolism 20040601

Title: Cotreatment with 17-allylamino-demethoxygeldanamycin and FLT-3 kinase inhibitor PKC412 is highly effective against human acute myelogenous leukemia cells with mutant FLT-3.

Journal: Cancer research 20040515

Title: Ubiquitination and proteasomal degradation of nucleophosmin-anaplastic lymphoma kinase induced by 17-allylamino-demethoxygeldanamycin: role of the co-chaperone carboxyl heat shock protein 70-interacting protein.

Journal: Cancer research 20040501

Title: Simultaneous inhibition of hsp 90 and the proteasome promotes protein ubiquitination, causes endoplasmic reticulum-derived cytosolic vacuolization, and enhances antitumor activity.

Journal: Molecular cancer therapeutics 20040501

Title: Clinical trials referral resource. Current clinical trials of 17-AG and 17-DMAG.

Journal: Oncology (Williston Park, N.Y.) 20040501

Title: Combinatorial attack on multistep oncogenesis by inhibiting the Hsp90 molecular chaperone.

Journal: Cancer letters 20040408

Title: 17-(Allylamino)-17-demethoxygeldanamycin activity in human melanoma models.

Journal: Anti-cancer drugs 20040401

Title: 17-Allylamino-17-demethoxygeldanamycin (17-AAG) is effective in down-regulating mutated, constitutively activated KIT protein in human mast cells.

Journal: Blood 20040201

Title: Altered states: selectively drugging the Hsp90 cancer chaperone.

Journal: Trends in molecular medicine 20040201

Title: Protein chaperones as anticancer therapy targets.

Journal: Clinical advances in hematology & oncology : H&O 20040201

Title: Adenine derived inhibitors of the molecular chaperone HSP90-SAR explained through multiple X-ray structures.

Journal: Bioorganic & medicinal chemistry letters 20040119

Title: Quantitative effects on c-Jun N-terminal protein kinase signaling determine synergistic interaction of cisplatin and 17-allylamino-17-demethoxygeldanamycin in colon cancer cell lines.

Journal: Molecular pharmacology 20040101

Title: Expression of the insulin-like growth factor I receptor and urokinase plasminogen activator in breast cancer is associated with poor survival: potential for intervention with 17-allylamino geldanamycin.

Journal: Cancer research 20040101

Title: Hsp90 inhibition depletes Chk1 and sensitizes tumor cells to replication stress.

Journal: The Journal of biological chemistry 20031226

Title: Additive interaction of oxaliplatin and 17-allylamino-17-demethoxygeldanamycin in colon cancer cell lines results from inhibition of nuclear factor kappaB signaling.

Journal: Cancer research 20031215

Title: Geldanamycin and 17-allylamino-17-demethoxygeldanamycin potentiate the in vitro and in vivo radiation response of cervical tumor cells via the heat shock protein 90-mediated intracellular signaling and cytotoxicity.

Journal: Cancer research 20031215

Title: Combination treatment with 17-N-allylamino-17-demethoxy geldanamycin and acute irradiation produces supra-additive growth suppression in human prostate carcinoma spheroids.

Journal: Cancer research 20031201

Title: Coadministration of the heat shock protein 90 antagonist 17-allylamino- 17-demethoxygeldanamycin with suberoylanilide hydroxamic acid or sodium butyrate synergistically induces apoptosis in human leukemia cells.

Journal: Cancer research 20031201

Title: Magnetic resonance spectroscopic pharmacodynamic markers of the heat shock protein 90 inhibitor 17-allylamino,17-demethoxygeldanamycin (17AAG) in human colon cancer models.

Journal: Journal of the National Cancer Institute 20031105

Title: Hormone-refractory breast cancer remains sensitive to the antitumor activity of heat shock protein 90 inhibitors.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20031015

Title: Overview: translating Hsp90 biology into Hsp90 drugs.

Journal: Current cancer drug targets 20031001

Title: Clinical development of 17-allylamino, 17-demethoxygeldanamycin.

Journal: Current cancer drug targets 20031001

Title: The clinical applications of heat shock protein inhibitors in cancer - present and future.

Journal: Current cancer drug targets 20031001

Title: FLT3 expressing leukemias are selectively sensitive to inhibitors of the molecular chaperone heat shock protein 90 through destabilization of signal transduction-associated kinases.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20031001

Title: Hsp90 as a therapeutic target in prostate cancer.

Journal: Seminars in oncology 20031001

Title: Cancer: the rules of attraction.

Journal: Nature 20030925

Title: A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors.

Journal: Nature 20030925

Title: Synergistic antileukemic interactions between 17-AAG and UCN-01 involve interruption of RAF/MEK- and AKT-related pathways.

Journal: Blood 20030901

Title: Enhanced cell killing induced by the combination of radiation and the heat shock protein 90 inhibitor 17-allylamino-17- demethoxygeldanamycin: a multitarget approach to radiosensitization.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20030901

Title: Biliary excretion of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) and metabolites by Fischer 344 rats.

Journal: Cancer chemotherapy and pharmacology 20030801

Title: The Hsp90 chaperone complex as a novel target for cancer therapy.

Journal: Annals of oncology : official journal of the European Society for Medical Oncology 20030801

Title: Medulloblastoma sensitivity to 17-allylamino-17-demethoxygeldanamycin requires MEK/ERKM.

Journal: The Journal of biological chemistry 20030704

Title: Regulation of 17-AAG-induced apoptosis: role of Bcl-2, Bcl-XL, and Bax downstream of 17-AAG-mediated down-regulation of Akt, Raf-1, and Src kinases.

Journal: Blood 20030701

Title: Geldanamycin and its 17-allylamino-17-demethoxy analogue antagonize the action of Cisplatin in human colon adenocarcinoma cells: differential caspase activation as a basis for interaction.

Journal: Cancer research 20030615

Title: Physiologically-based pharmacokinetics and molecular pharmacodynamics of 17-(allylamino)-17-demethoxygeldanamycin and its active metabolite in tumor-bearing mice.

Journal: Journal of pharmacokinetics and pharmacodynamics 20030601

Title: Development of small molecule Hsp90 inhibitors: utilizing both forward and reverse chemical genomics for drug identification.

Journal: Current medicinal chemistry 20030501

Title: Inhibition of heat shock protein 90 function down-regulates Akt kinase and sensitizes tumors to Taxol.

Journal: Cancer research 20030501

Title: Cross-resistance of imatinib mesylate and 17-AAG in imatinib-resistant cells that overexpress BCR-ABL.

Journal: British journal of haematology 20030501

Title: Inhibition of telomerase activity by geldanamycin and 17-allylamino, 17-demethoxygeldanamycin in human melanoma cells.

Journal: Carcinogenesis 20030501

Title: ErbB2 degradation mediated by the co-chaperone protein CHIP.

Journal: The Journal of biological chemistry 20030418

Title: 17AAG: low target binding affinity and potent cell activity--finding an explanation.

Journal: Molecular cancer therapeutics 20030201

Title: Auditing the pharmacological accounts for Hsp90 molecular chaperone inhibitors: unfolding the relationship between pharmacokinetics and pharmacodynamics.

Journal: Molecular cancer therapeutics 20030201

Title: Yeast is selectively hypersensitised to heat shock protein 90 (Hsp90)-targetting drugs with heterologous expression of the human Hsp90beta, a property that can be exploited in screens for new Hsp90 chaperone inhibitors.

Journal: Gene 20030102

Title: [Molecular chaperone HSP90 as a novel target for cancer chemotherapy].

Journal: Nihon yakurigaku zasshi. Folia pharmacologica Japonica 20030101

Title: The role of functional and molecular imaging in cancer drug discovery and development.

Journal: The British journal of radiology 20030101

Title: Synthetic lethality: killing cancer with cancer.

Journal: Journal of the National Cancer Institute 20021120

Title: Challenges of PK/PD measurements in modern drug development.

Journal: European journal of cancer (Oxford, England : 1990) 20021101

Title: Molecular characterization and sensitivity of STI-571 (imatinib mesylate, Gleevec)-resistant, Bcr-Abl-positive, human acute leukemia cells to SRC kinase inhibitor PD180970 and 17-allylamino-17-demethoxygeldanamycin.

Journal: Cancer research 20021015

Title: Heat shock protein and proteasome targeting agents.

Journal: Hematology/oncology clinics of North America 20021001

Title: Heat shock protein inhibitor shows antitumor activity.

Journal: Journal of the National Cancer Institute 20020821

Title: Degradation of HER2 by ansamycins induces growth arrest and apoptosis in cells with HER2 overexpression via a HER3, phosphatidylinositol 3'-kinase-AKT-dependent pathway.

Journal: Cancer research 20020601

Title: Heat shock protein 90 inhibition by 17-allylamino-17- demethoxygeldanamycin: a novel therapeutic approach for treating hormone-refractory prostate cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20020501

Title: 17-Allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20020501

Title: Nucleophosmin-anaplastic lymphoma kinase (NPM-ALK), a novel Hsp90-client tyrosine kinase: down-regulation of NPM-ALK expression and tyrosine phosphorylation in ALK(+) CD30(+) lymphoma cells by the Hsp90 antagonist 17-allylamino,17-demethoxygeldanamycin.

Journal: Cancer research 20020301

Title: Suppressive effects of ansamycins on inducible nitric oxide synthase expression and the development of experimental autoimmune encephalomyelitis.

Journal: Journal of neuroscience research 20020215

Title: Ansamycin antibiotics inhibit Akt activation and cyclin D expression in breast cancer cells that overexpress HER2.

Journal: Oncogene 20020214

Title: HSP90 as a new therapeutic target for cancer therapy: the story unfolds.

Journal: Expert opinion on biological therapy 20020101

Title: Combining cytotoxics and 17-allylamino, 17-demethoxygeldanamycin: sequence and tumor biology matters. Commentary re: P. Münster et al., Modulation of Hsp90 function by ansamycins sensitizes breast cancer cells to chemotherapy-induced apoptosis in an RB- and schedule-dependent manner. Clin. Cancer Res., 7: 2228-2236, 2001.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20010801

Title: Modulation of Hsp90 function by ansamycins sensitizes breast cancer cells to chemotherapy-induced apoptosis in an RB- and schedule-dependent manner. See: E. A. Sausville, Combining cytotoxics and 17-allylamino, 17-demethoxygeldanamycin: sequence and tumor biology matters, Clin. Cancer Res., 7: 2155-2158, 2001.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20010801

Title: Inhibition of signal transduction by the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin results in cytostasis and apoptosis.

Journal: Cancer research 20010515

Title: Disruption of the EF-2 kinase/Hsp90 protein complex: a possible mechanism to inhibit glioblastoma by geldanamycin.

Journal: Cancer research 20010515

Title: Measurement of the novel antitumor agent 17-(allylamino)-17-demethoxygeldanamycin in human plasma by high-performance liquid chromatography.

Journal: Journal of chromatography. B, Biomedical sciences and applications 20010505

Title: LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family.

Journal: Bioorganic & medicinal chemistry letters 20010409

Title: Inhibition of heat shock protein 90 function by ansamycins causes the morphological and functional differentiation of breast cancer cells.

Journal: Cancer research 20010401

Title: Plasma pharmacokinetics and tissue distribution of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) in CD2F1 mice1.

Journal: Cancer chemotherapy and pharmacology 20010401

Title: Magnetic resonance detects changes in phosphocholine associated with Ras activation and inhibition in NIH 3T3 cells.

Journal: British journal of cancer 20010301

Title: Geldanamycin and its analogue 17-allylamino-17-demethoxygeldanamycin lowers Bcr-Abl levels and induces apoptosis and differentiation of Bcr-Abl-positive human leukemic blasts.

Journal: Cancer research 20010301

Title: Solit DB, et al. 17-Allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts.Clin Cancer Res, 2002, 8(5), 986-993.

Title: Raja, Srikumar M., et al. 17-AAG induces enhanced ubiquitinylation and lysosomal pathway-dependent ErbB2 degradation and cytotoxicity in ErbB2-overexpressing breast cancer cells. Cancer Biology & Therapy (2008), 7(10), 163

Title: Zhang J, et al. The heat shock protein 90 inhibitor 17-AAG suppresses growth and induces apoptosis in human cholangiocarcinoma cells.Clin Exp Med. 2012 Sep 7.

Title: Newman B, et al. HSP90 Inhibitor 17-AAG Selectively Eradicates Lymphoma Stem Cells.Cancer Res. 2012 Sep 1;72(17):4551-61. Epub 2012 Jun 29.

Title: Kamal A, et al. A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors. Nature. 2003 Sep 25;425(6956):407-10.

Title: Enomoto A, et al. The HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin modulates radiosensitivity by downregulating serine/threonine kinase 38 via Sp1 inhibition. Eur J Cancer. 2013 Nov;49(16):3547-58.

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Tags:75747-14-7 Molecular Formula|75747-14-7 MDL|75747-14-7 SMILES|75747-14-7 17-AAG