Title: The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.
Journal: Journal of medicinal chemistry 20150108
Title: Direct and indirect targeting of MYC to treat acute myeloid leukemia.
Journal: Cancer chemotherapy and pharmacology 20150101
Title: Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
Journal: Journal of medicinal chemistry 20131024
Title: The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents.
Journal: Journal of medicinal chemistry 20130808
Title: Identification of potent Yes1 kinase inhibitors using a library screening approach.
Journal: Bioorganic & medicinal chemistry letters 20130801
Title: A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
Journal: The Biochemical journal 20130415
Title: Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors.
Journal: Journal of medicinal chemistry 20120913
Title: Co-treatment with vorinostat synergistically enhances activity of Aurora kinase inhibitor against human breast cancer cells.
Journal: Breast cancer research and treatment 20120901
Title: Activation of Aurora-A is essential for neuronal migration via modulation of microtubule organization.
Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20120808
Title: Repression of cancer cell senescence by PKCι.
Journal: Oncogene 20120802
Title: Gadd45a transcriptional induction elicited by the Aurora kinase inhibitor MK-0457 in Bcr-Abl-expressing cells is driven by Oct-1 transcription factor.
Journal: Leukemia research 20120801
Title: Synthesis, biological evaluation, and molecular docking studies of N,1,3-triphenyl-1H-pyrazole-4-carboxamide derivatives as anticancer agents.
Journal: Bioorganic & medicinal chemistry letters 20120601
Title: Acute sensitization of colon cancer cells to inflammatory cytokines by prophase arrest.
Journal: Biochemical pharmacology 20120501
Title: In vitro drug metabolism by C-terminally truncated human flavin-containing monooxygenase 3.
Journal: Biochemical pharmacology 20120215
Title: Targeting aurora kinases: a novel approach to curb the growth & chemoresistance of androgen refractory prostate cancer.
Journal: Current cancer drug targets 20120201
Title: Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen.
Journal: ACS chemical biology 20120120
Title: Histone H3 covalent modifications driving response of BCR-ABL1+ cells sensitive and resistant to imatinib to Aurora kinase inhibitor MK-0457.
Journal: British journal of haematology 20120101
Title: Vincristine potentiates the anti-proliferative effect of an aurora kinase inhibitor, VE-465, in myeloid leukemia cells.
Journal: Biochemical pharmacology 20111215
Title: Mutants of protein kinase A that mimic the ATP-binding site of Aurora kinase.
Journal: The Biochemical journal 20111115
Title: Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.
Journal: Nature biotechnology 20111101
Title: Comprehensive analysis of kinase inhibitor selectivity.
Journal: Nature biotechnology 20111030
Title: An integrated chemical biology approach identifies specific vulnerability of Ewing's sarcoma to combined inhibition of Aurora kinases A and B.
Journal: Molecular cancer therapeutics 20111001
Title: Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors.
Journal: Bioorganic & medicinal chemistry letters 20110915
Title: A novel cell-based, high-content assay for phosphorylation of Lats2 by Aurora A.
Journal: Journal of biomolecular screening 20110901
Title: Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.
Journal: European journal of medicinal chemistry 20110601
Title: Combining histone deacetylase inhibitor vorinostat with aurora kinase inhibitors enhances lymphoma cell killing with repression of c-Myc, hTERT, and microRNA levels.
Journal: Cancer research 20110601
Title: VX680 binding in Aurora A: π-π interactions involving the conserved aromatic amino acid of the flexible glycine-rich loop.
Journal: The journal of physical chemistry. A 20110428
Title: Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class.
Journal: Journal of medicinal chemistry 20110414
Title: Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase.
Journal: Journal of medicinal chemistry 20110113
Title: Inhibition of mitotic kinase Aurora suppresses Akt-1 activation and induces apoptotic cell death in all-trans retinoid acid-resistant acute promyelocytic leukemia cells.
Journal: Journal of translational medicine 20110101
Title: Inhibition of proliferation, viability, migration and invasion of gastric cancer cells by Aurora-A deletion.
Journal: Asian Pacific journal of cancer prevention : APJCP 20110101
Title: Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines.
Journal: Cancer research 20101201
Title: Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.
Journal: Chemistry & biology 20101124
Title: Efficacy of MK-0457 and in combination with vorinostat against Philadelphia chromosome positive acute lymphoblastic leukemia cells.
Journal: Annals of hematology 20101101
Title: Evaluation of an Actinomycin D/VX-680 aurora kinase inhibitor combination in p53-based cyclotherapy.
Journal: Oncotarget 20101101
Title: Combination of nutlin-3 and VX-680 selectively targets p53 mutant cells with reversible effects on cells expressing wild-type p53.
Journal: Cell death and differentiation 20100901
Title: A type-II kinase inhibitor capable of inhibiting the T315I 'gatekeeper' mutant of Bcr-Abl.
Journal: Journal of medicinal chemistry 20100812
Title: 3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors.
Journal: Bioorganic & medicinal chemistry letters 20100801
Title: Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification.
Journal: Journal of medicinal chemistry 20100708
Title: Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.
Journal: Journal of medicinal chemistry 20100527
Title: Activity of the Aurora kinase inhibitor VX-680 against Bcr/Abl-positive acute lymphoblastic leukemias.
Journal: Molecular cancer therapeutics 20100501
Title: Targets and effectors of the cellular response to aurora kinase inhibitor MK-0457 (VX-680) in imatinib sensitive and resistant chronic myelogenous leukemia.
Journal: Biochemical pharmacology 20100301
Title: Inhibition of the aurora kinases suppresses in vitro NT2-D1 cell growth and tumorigenicity.
Journal: The Journal of endocrinology 20100201
Title: In vitro anti-myeloma activity of the Aurora kinase inhibitor VE-465.
Journal: British journal of haematology 20091201
Title: Overcoming resistance in chronic myelogenous leukemia.
Journal: Leukemia & lymphoma 20091101
Title: The Aurora Kinase in Trypanosoma brucei plays distinctive roles in metaphase-anaphase transition and cytokinetic initiation.
Journal: PLoS pathogens 20090901
Title: The discovery of the potent aurora inhibitor MK-0457 (VX-680).
Journal: Bioorganic & medicinal chemistry letters 20090701
Title: Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks.
Journal: The Journal of biological chemistry 20090605
Title: Multitargeted sequential therapy with MK-0457 and dasatinib followed by stem cell transplantation for T315I mutated chronic myeloid leukemia.
Journal: Leukemia research 20090601
Title: Discovery and development of aurora kinase inhibitors as anticancer agents.
Journal: Journal of medicinal chemistry 20090514
Title: Biochemical characterization of GSK1070916, a potent and selective inhibitor of Aurora B and Aurora C kinases with an extremely long residence time1.
Journal: The Biochemical journal 20090513
Title: Short and long-term tumor cell responses to Aurora kinase inhibitors.
Journal: Experimental cell research 20090415
Title: Identification of genes that confer tumor cell resistance to the aurora B kinase inhibitor, AZD1152.
Journal: The pharmacogenomics journal 20090401
Title: Mechanism of MK-0457 efficacy against BCR-ABL positive leukemia cells.
Journal: Biochemical and biophysical research communications 20090320
Title: [Recent advance in the study of novel anti-tumor targets and drugs--aurora kinase and Pin1].
Journal: Yao xue xue bao = Acta pharmaceutica Sinica 20090301
Title: Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.
Journal: Journal of medicinal chemistry 20090122
Title: Aurora-A down-regulates IkappaBalpha via Akt activation and interacts with insulin-like growth factor-1 induced phosphatidylinositol 3-kinase pathway for cancer cell survival.
Journal: Molecular cancer 20090101
Title: Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.
Journal: Journal of medicinal chemistry 20081225
Title: Aurora A is essential for early embryonic development and tumor suppression.
Journal: The Journal of biological chemistry 20081114
Title: Concomitant inhibition of Mdm2-p53 interaction and Aurora kinases activates the p53-dependent postmitotic checkpoints and synergistically induces p53-mediated mitochondrial apoptosis along with reduced endoreduplication in acute myelogenous leukemia.
Journal: Blood 20081001
Title: Modulation of kinase-inhibitor interactions by auxiliary protein binding: crystallography studies on Aurora A interactions with VX-680 and with TPX2.
Journal: Protein science : a publication of the Protein Society 20081001
Title: Inhibition of Aurora-A suppresses epithelial-mesenchymal transition and invasion by downregulating MAPK in nasopharyngeal carcinoma cells.
Journal: Carcinogenesis 20081001
Title: Cotreatment with vorinostat enhances activity of MK-0457 (VX-680) against acute and chronic myelogenous leukemia cells.
Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20081001
Title: Targeting aurora kinase with MK-0457 inhibits ovarian cancer growth.
Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20080901
Title: Vorinostat synergistically potentiates MK-0457 lethality in chronic myelogenous leukemia cells sensitive and resistant to imatinib mesylate.
Journal: Blood 20080801
Title: [Novel medical treatment modalities in hematology].
Journal: Ugeskrift for laeger 20080609
Title: Activity of a novel Aurora kinase inhibitor against the T315I mutant form of BCR-ABL: in vitro and in vivo studies.
Journal: Cancer science 20080601
Title: Effects of the Aurora kinase inhibitor VX-680 on anaplastic thyroid cancer-derived cell lines.
Journal: Endocrine-related cancer 20080601
Title: Aurora kinase inhibitory VX-680 increases Bax/Bcl-2 ratio and induces apoptosis in Aurora-A-high acute myeloid leukemia.
Journal: Blood 20080301
Title: Aurora kinase A inhibitors: identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold.
Journal: Bioorganic & medicinal chemistry letters 20080301
Title: Spatio-temporal expression patterns of aurora kinases a, B, and C and cytoplasmic polyadenylation-element-binding protein in bovine oocytes during meiotic maturation.
Journal: Biology of reproduction 20080201
Title: A quantitative analysis of kinase inhibitor selectivity.
Journal: Nature biotechnology 20080101
Title: Inhibitors of ABL and the ABL-T315I mutation.
Journal: Current topics in medicinal chemistry 20080101
Title: Aurora kinase inhibitors synergize with paclitaxel to induce apoptosis in ovarian cancer cells.
Journal: Journal of translational medicine 20080101
Title: The selectivity of protein kinase inhibitors: a further update.
Journal: The Biochemical journal 20071215
Title: [Acute lymphoblastic leukemia with Philadelphia chromosome: treatment with kinase inhibitors].
Journal: Bulletin du cancer 20071001
Title: Sequential ABL kinase inhibitor therapy selects for compound drug-resistant BCR-ABL mutations with altered oncogenic potency.
Journal: The Journal of clinical investigation 20070904
Title: Hepatic metabolism of MK-0457, a potent aurora kinase inhibitor: interspecies comparison and role of human cytochrome P450 and flavin-containing monooxygenase.
Journal: Drug metabolism and disposition: the biological fate of chemicals 20070901
Title: Transforming acidic coiled-coil 3 and Aurora-A interact in human thyrocytes and their expression is deregulated in thyroid cancer tissues.
Journal: Endocrine-related cancer 20070901
Title: Structural basis for potent inhibition of the Aurora kinases and a T315I multi-drug resistant mutant form of Abl kinase by VX-680.
Journal: Cancer letters 20070628
Title: [Novel anti-CML agents beyond imatinib].
Journal: [Rinsho ketsueki] The Japanese journal of clinical hematology 20070601
Title: Targeted therapy and the T315I mutation in Philadelphia-positive leukemias.
Journal: Haematologica 20070401
Title: New blood cancer therapies under study.
Journal: JAMA 20070207
Title: With targeted drugs, chronic myelogenous leukemia therapy may follow HIV's model.
Journal: Journal of the National Cancer Institute 20070207
Title: MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation.
Journal: Blood 20070115
Title: Aurora kinase inhibition downregulates NF-kappaB and sensitises tumour cells to chemotherapeutic agents.
Journal: Biochemical and biophysical research communications 20070105
Title: Analysis of mitotic phosphorylation of borealin.
Journal: BMC cell biology 20070101
Title: Microsphere-based protease assays and screening application for lethal factor and factor Xa.
Journal: Cytometry. Part A : the journal of the International Society for Analytical Cytology 20060501
Title: Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.
Journal: Journal of medicinal chemistry 20060209
Title: Structure of the kinase domain of an imatinib-resistant Abl mutant in complex with the Aurora kinase inhibitor VX-680.
Journal: Cancer research 20060115
Title: Anticancer Drug Discovery and Development - SRI's Seventh Annual Summit.
Journal: IDrugs : the investigational drugs journal 20051001
Title: Dawn of Aurora kinase inhibitors as anticancer drugs.
Journal: Expert opinion on investigational drugs 20040901
Title: VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo.
Journal: Nature medicine 20040301
Title: Harrington EA, et al. VX-680, a potent and selective smallmolecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nat Med. 2004; 10:262-7.
Title: Salah E, et al. Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class.J Med Chem. 2011 Apr 14;54(7):2359-67. Epub 2011 Mar 18.
Title: Arlot-Bonnemains Y, et al. Effects of the Aurora kinase inhibitor VX-680 on anaplastic thyroid cancer-derived cell lines. Endocr Relat Cancer. 2008 Jun;15(2):559-68
