Design, synthesis, and in vitro evaluation of a fluorescently labeled irreversible inhibitor of the catalytic subunit of cAMP-dependent protein kinase (PKACα)
Author:
Affiliation:
1. Department of Medicinal Chemistry
2. Virginia Commonwealth University
3. Richmond
4. USA
5. Massey Cancer Center
6. Institute for Structural Biology
7. Drug Discovery
8. and Development
Abstract
A new fluorescent-labeled inhibitor for PKACα was developed that potently inhibits the kinase (IC50 = 11.8 nM), is >100-fold selective for PKACα, and irreversibly labels Cys199.
Funder
National Cancer Institute
American Cancer Society
Publisher
Royal Society of Chemistry (RSC)
Subject
Organic Chemistry,Physical and Theoretical Chemistry,Biochemistry
Link
http://pubs.rsc.org/en/content/articlepdf/2016/OB/C6OB00529B
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