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

被引：0
|
作者：
Tinghu Zhang
Nicholas Kwiatkowski
Calla M Olson
Sarah E Dixon-Clarke
Brian J Abraham
Ann K Greifenberg
Scott B Ficarro
Jonathan M Elkins
Yanke Liang
Nancy M Hannett
Theresa Manz
Mingfeng Hao
Bartlomiej Bartkowiak
Arno L Greenleaf
Jarrod A Marto
Matthias Geyer
Alex N Bullock
Richard A Young
Nathanael S Gray
机构：
[1] Dana–Farber Cancer Institute,Department of Cancer Biology
[2] Harvard Medical School,Department of Biological Chemistry and Molecular Pharmacology
[3] Whitehead Institute for Biomedical Research,Department of Structural Immunology
[4] Structural Genomics Consortium,Department of Pharmacy
[5] University of Oxford,Department of Biochemistry
[6] Institute of Innate Immunity,Department of Biology
[7] University of Bonn,undefined
[8] Center of Advanced European Studies and Research,undefined
[9] Bonn,undefined
[10] Blais Proteomics Center,undefined
[11] Dana–Farber Cancer Institute,undefined
[12] Pharmaceutical and Medicinal Chemistry,undefined
[13] Saarland University,undefined
[14] Duke University Medical Center,undefined
[15] Massachusetts Institute of Technology,undefined
来源：
Nature Chemical Biology | 2016年 / 12卷
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摘要：
A small molecule inhibits CDK12 and CDK13 activity through covalent modification of Cys residues and reveals a role of the two kinases in regulating Pol II processivity and super-enhancer-driven transcription factor and DNA damage response gene expression.[graphic not available: see fulltext]
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页码：876 / 884
页数：8
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