Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation

Cyclin-dependent kinase 9 (CDK9), an important regulator of transcriptional elongation, is a promising target for cancer therapy, particularly for cancers driven by transcriptional dysregulation. We characterized NVP-2, a selective ATP-competitive CDK9 inhibitor, and THAL-SNS-032, a selective CDK9 d...

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Bibliographic Details
Published in:	Nature chemical biology Vol. 14; no. 2; p. 163
Main Authors:	Olson, Calla M, Jiang, Baishan, Erb, Michael A, Liang, Yanke, Doctor, Zainab M, Zhang, Zinan, Zhang, Tinghu, Kwiatkowski, Nicholas, Boukhali, Myriam, Green, Jennifer L, Haas, Wilhelm, Nomanbhoy, Tyzoon, Fischer, Eric S, Young, Richard A, Bradner, James E, Winter, Georg E, Gray, Nathanael S
Format:	Journal Article
Language:	English
Published:	United States Nature Publishing Group 01.02.2018
Subjects:	Apoptosis Cancer Cell Line, Tumor Cell Proliferation Conjugation Crystallography, X-Ray Cyclin-dependent kinase 9 Cyclin-Dependent Kinase 9 - antagonists & inhibitors Cyclin-Dependent Kinase 9 - chemistry Cyclin-dependent kinases Cytotoxicity Degradation Elongation Humans Inhibitory Concentration 50 Kinases Ligands Oxazoles - pharmacology Peptide Hydrolases - chemistry Pharmacology Phosphorylation Protein Binding Protein Conformation Protein Kinase Inhibitors - pharmacology Proteomics Thalidomide Thalidomide - pharmacology Thiazoles - pharmacology Transcription elongation Ubiquitin Ubiquitin-protein ligase
ISSN:	1552-4450, 1552-4469, 1552-4469
Online Access:	Get full text
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