PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

Proceedings of the National Academy of Sciences of the United States of America

Volumn 113, Issue 26, 2016, Pages 7124-7129

  Raina, Kanak ^a   Lu, Jing ^a   Qian, Yimin ^a   Altieri, Martha ^a   Gordon, Deborah ^a   Rossi, Ann Marie K ^a   Wang, Jing ^a   Chen, Xin ^a   Dong, Hanqing ^a   Siu, Kam ^a   Winkler, James D ^a   Crew, Andrew P ^a   Crews, Craig M ^b,c   Coleman, Kevin G ^a  

^a Arvinas Inc   (United States)

^b YALE UNIVERSITY   (United States)

^c YALE UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

BET; BRD4; Prostate; PROTAC; Protein degradation

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; 4 (4 CHLOROPHENYL) N (4 HYDROXYPHENYL) 2,3,9 TRIMETHYL 6H THIENO[3,2 F][1,2,4]TRIAZOLO[4,3 A][1,4]DIAZEPINE 6 ACETAMIDE; ANDROGEN RECEPTOR; ARV 771; BROMODOMAIN AND EXTRATERMINAL PROTEIN; BROMODOMAIN INHIBITOR; ENZALUTAMIDE; PROTEIN; UNCLASSIFIED DRUG; ANTINEOPLASTIC AGENT; BRD2 PROTEIN, HUMAN; BRD3 PROTEIN, HUMAN; BRD4 PROTEIN, HUMAN; NUCLEAR PROTEIN; PROTEIN SERINE THREONINE KINASE; RNA BINDING PROTEIN; TRANSCRIPTION FACTOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; APOPTOSIS; ARTICLE; CANCER CELL; CANCER INHIBITION; CASTRATION RESISTANT PROSTATE CANCER; CELL PROLIFERATION; CHIMERA; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG STRUCTURE; IC50; IN VIVO STUDY; MALE; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN DEGRADATION; PROTEOLYSIS TARGETING CHIMERA; SIGNAL TRANSDUCTION; TUMOR REGRESSION; TUMOR XENOGRAFT; ANIMAL; DRUG EFFECTS; GENETICS; HUMAN; METABOLISM; PROSTATIC NEOPLASMS, CASTRATION-RESISTANT; TUMOR CELL LINE;

ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; HUMANS; MALE; MICE; NUCLEAR PROTEINS; PROSTATIC NEOPLASMS, CASTRATION-RESISTANT; PROTEIN-SERINE-THREONINE KINASES; PROTEOLYSIS; RECEPTORS, ANDROGEN; RNA-BINDING PROTEINS; SIGNAL TRANSDUCTION; TRANSCRIPTION FACTORS;

EID: 84976614642     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.1521738113     Document Type: Article

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