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

关键词：

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中图分类号：

学科分类号：

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]

引用

页码：876 / 884

页数：8

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