AZD5153: A novel bivalent BET bromodomain inhibitor highly active against hematologic malignancies

Molecular Cancer Therapeutics

Volumn 15, Issue 11, 2016, Pages 2563-2574

  Rhyasen, Garrett W ^a   Hattersley, Maureen M ^a   Yao, Yi ^a   Dulak, Austin ^a   Wang, Wenxian ^a   Petteruti, Philip ^a   Dale, Ian L ^a   Boiko, Scott ^a   Cheung, Tony ^a   Zhang, Jingwen ^a   Wen, Shenghua ^a   Castriotta, Lillian ^a   Lawson, Deborah ^a   Collins, Michael ^a   Bao, Larry ^a   Ahdesmaki, Miika J ^a   Walker, Graeme ^a   O'Connor, Greg ^a   Yeh, Tammie C ^a   Rabow, Alfred A ^a   Dry, Jonathan R ^a   Reimer, Corinne ^a   Lyne, Paul ^a   Mills, Gordon B ^b   Fawell, Stephen E ^a   Waring, Michael J ^a   Zinda, Michael ^a   Clark, Edwin ^a   Chen, Huawei ^a   more..

^a ASTRAZENECA   (United Kingdom)

^b UNIVERSITY OF TEXAS MD ANDERSON CANCER CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 (4 CHLOROPHENYL) 2,3,9 TRIMETHYL 6H THIENO[3,2 F][1,2,4]TRIAZOLO[4,3 A][1,4]DIAZEPINE 6 ACETIC ACID TERT BUTYL ESTER; 6 (4 CHLOROPHENYL) N ETHYL 8 METHOXY 1 METHYL 4H [1,2,4]TRIAZOLO[4,3 A][1,4]BENZODIAZEPINE 4 ACETAMIDE; AZD 5153; BROMODOMAIN INHIBITOR; MESSENGER RNA; MYC PROTEIN; UNCLASSIFIED DRUG; ANTINEOPLASTIC AGENT; BIOLOGICAL MARKER; BRD4 PROTEIN, HUMAN; NUCLEAR PROTEIN; PROTEIN BINDING; TARGET OF RAPAMYCIN KINASE; TRANSCRIPTION FACTOR; TRANSCRIPTION FACTOR E2F;

ACUTE MYELOBLASTIC LEUKEMIA; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; APOPTOSIS; ARTICLE; BINDING AFFINITY; CELL CYCLE PROGRESSION; CELL SURVIVAL; CELL VIABILITY; CELL VIABILITY ASSAY; CONTROLLED STUDY; CRYSTAL STRUCTURE; DOWN REGULATION; DRUG BLOOD LEVEL; DRUG EFFICACY; ENHANCER REGION; FEMALE; FLOW CYTOMETRY; HEMATOLOGIC MALIGNANCY; IC50; IMMUNOFLUORESCENCE TEST; IN VIVO STUDY; LARGE CELL LYMPHOMA; MOUSE; MULTIPLE MYELOMA; NONHUMAN; PRIORITY JOURNAL; QUANTITATIVE ANALYSIS; RNA SEQUENCE; TUMOR MODEL; TUMOR REGRESSION; ULTRACENTRIFUGATION; WEIGHT REDUCTION; WESTERN BLOTTING; X RAY CRYSTALLOGRAPHY; ANIMAL; ANTAGONISTS AND INHIBITORS; CELL PROLIFERATION; CHEMISTRY; DISEASE MODEL; DOSE RESPONSE; DRUG EFFECTS; DRUG SCREENING; GENE EXPRESSION PROFILING; GENE EXPRESSION REGULATION; GENETICS; HEMATOLOGIC NEOPLASMS; HUMAN; METABOLISM; MOLECULARLY TARGETED THERAPY; PATHOLOGY; SIGNAL TRANSDUCTION; TUMOR CELL LINE; TUMOR VOLUME;

ANIMALS; ANTINEOPLASTIC AGENTS; APOPTOSIS; BIOMARKERS; CELL LINE, TUMOR; CELL PROLIFERATION; CELL SURVIVAL; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; E2F TRANSCRIPTION FACTORS; FEMALE; GENE EXPRESSION PROFILING; GENE EXPRESSION REGULATION, NEOPLASTIC; HEMATOLOGIC NEOPLASMS; HUMANS; MICE; MOLECULAR TARGETED THERAPY; NUCLEAR PROTEINS; PROTEIN BINDING; PROTO-ONCOGENE PROTEINS C-MYC; SIGNAL TRANSDUCTION; TOR SERINE-THREONINE KINASES; TRANSCRIPTION FACTORS; TUMOR BURDEN; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84995428342     PISSN: 15357163     EISSN: 15388514     Source Type: Journal    
DOI: 10.1158/1535-7163.MCT-16-0141     Document Type: Article

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