Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors

Nature Chemical Biology

Volumn 12, Issue 10, 2016, Pages 876-884

  Zhang, Tinghu ^a,b   Kwiatkowski, Nicholas ^a,c   Olson, Calla M ^a,b   Dixon Clarke, Sarah E ^d   Abraham, Brian J ^c   Greifenberg, Ann K ^e,f   Ficarro, Scott B ^a,b   Elkins, Jonathan M ^d   Liang, Yanke ^a,b   Hannett, Nancy M ^c   Manz, Theresa ^a,g   Hao, Mingfeng ^a,b   Bartkowiak, Bartlomiej ^h   Greenleaf, Arno L ^h   Marto, Jarrod A ^a,b   Geyer, Matthias ^e,f   Bullock, Alex N ^d   Young, Richard A ^c,i   Gray, Nathanael S ^a,b  

^a DANA FARBER CANCER INSTITUTE   (United States)

^b HARVARD MEDICAL SCHOOL   (United States)

^c WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCH   (United States)

^d UNIVERSITY OF OXFORD   (United Kingdom)

^e UNIVERSITY OF BONN   (Germany)

^f CENTER OF ADVANCED EUROPEAN STUDIES AND RESEARCH CAESAR   (Germany)

^g SAARLAND UNIVERSITY   (Germany)

^h DUKE UNIVERSITY MEDICAL CENTER   (United States)

ⁱ MASSACHUSETTS INSTITUTE OF TECHNOLOGY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLIN DEPENDENT KINASE 12 INHIBITOR; CYCLIN DEPENDENT KINASE 13 INHIBITOR; CYCLIN DEPENDENT KINASE INHIBITOR; CYSTEINE; RNA POLYMERASE II; TRANSCRIPTION FACTOR; UNCLASSIFIED DRUG; ANILIDE; CDK12 PROTEIN, HUMAN; CDK13 PROTEIN, HUMAN; CYCLIN DEPENDENT KINASE; CYCLIN DEPENDENT KINASE 1; PROTEIN KINASE INHIBITOR; PYRIMIDINE DERIVATIVE; THZ531;

APOPTOSIS; ARTICLE; CRYSTALLIZATION; DNA DAMAGE; ENZYME ACTIVITY; GENE EXPRESSION; HUMAN; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN PHOSPHORYLATION; PROTEIN TARGETING; TRANSCRIPTION ELONGATION; ANTAGONISTS AND INHIBITORS; CELL DEATH; CHEMISTRY; DRUG EFFECTS; METABOLISM; SYNTHESIS;

ANILIDES; CDC2 PROTEIN KINASE; CELL DEATH; CYCLIN-DEPENDENT KINASES; CYSTEINE; DNA DAMAGE; HUMANS; PROTEIN KINASE INHIBITORS; PYRIMIDINES;

EID: 84984637726     PISSN: 15524450     EISSN: 15524469     Source Type: Journal    
DOI: 10.1038/nchembio.2166     Document Type: Article

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