Biophysical investigation and conformational analysis of p38α kinase inhibitor doramapimod and its analogues
Author:
Affiliation:
1. Institute of Organic Chemistry and Chemical Biology
2. Center for Biomolecular Magnetic Resonance (BMRZ)
3. Johann Wolfgang Goethe-University Frankfurt
4. D-60438 Frankfurt am Main
5. Germany
Abstract
Doramapimod (BIRB 796) is a potent inhibitor of p38α nitrogen-activated protein kinase. By using biophysical methods, a clear correlation between kinase binding and the torsion angle θ of doramapimod analogues was found, highlighting the importance of inhibitor conformation for protein binding.
Publisher
Royal Society of Chemistry (RSC)
Subject
Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry
Link
http://pubs.rsc.org/en/content/articlepdf/2016/MD/C6MD00262E
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