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