Discovery and resistance mechanism of a selective CDK12 degrader

Cyclin-dependent kinase 12 (CDK12) is an emerging therapeutic target due to its role in regulating transcription of DNA-damage response (DDR) genes. However, development of selective small molecules targeting CDK12 has been challenging due to the high degree of homology between kinase domains of CDK...

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Veröffentlicht in:	Nature chemical biology Jg. 17; H. 6; S. 675 - 683
Hauptverfasser:	Jiang, Baishan, Gao, Yang, Che, Jianwei, Lu, Wenchao, Kaltheuner, Ines H., Dries, Ruben, Kalocsay, Marian, Berberich, Matthew J., Jiang, Jie, You, Inchul, Kwiatkowski, Nicholas, Riching, Kristin M., Daniels, Danette L., Sorger, Peter K., Geyer, Matthias, Zhang, Tinghu, Gray, Nathanael S.
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	New York Nature Publishing Group US 01.06.2021 Nature Publishing Group
Schlagworte:	631/337/572 631/67/1059 631/92/275 631/92/613 Adenosine diphosphate Adenylation Animals Biochemical Engineering Biochemistry Bioorganic Chemistry Cell Biology Chemistry Chemistry and Materials Science Chemistry/Food Science Chronic exposure Cyclin-dependent kinase Cyclin-dependent kinases Cyclin-Dependent Kinases - drug effects Degradation Deoxyribonucleic acid DNA DNA damage DNA Damage - genetics Domains Drug Design Drug Discovery Drug Resistance Genes Homology Humans Kinases Molting Mutation Poly A - metabolism Poly Adenosine Diphosphate Ribose - metabolism Poly(ADP-ribose) Poly(ADP-ribose) polymerase Protein Kinase Inhibitors - pharmacology Proteomics Ribose Transcription Tumor cells
ISSN:	1552-4450, 1552-4469, 1552-4469
Online-Zugang:	Volltext
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