Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8.

ACS Med Chem Lett

Department of Discovery Chemistry, Department of Translational Oncology, Department of Structural Biology, Department of Small Molecule Biochemical Pharmacology, Department of Pathology, Department of Drug Metabolism, and Department of Protein Chemistry, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.

Published: June 2016

Using Sorafenib as a starting point, a series of potent and selective inhibitors of CDK8 was developed. When cocrystallized with CDK8 and cyclin C, these compounds exhibit a Type-II (DMG-out) binding mode.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4904263PMC
http://dx.doi.org/10.1021/acsmedchemlett.6b00044DOI Listing

Publication Analysis

Top Keywords

series potent
8
potent selective
8
inhibitors cdk8
8
design development
4
development series
4
selective type
4
type inhibitors
4
cdk8 sorafenib
4
sorafenib starting
4
starting point
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!