| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372486 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
MK2 is a Ser/Thr kinase of significant interest as an anti-inflammatory drug discovery target. Here we describe the development of in vitro tools for the identification and characterization of MK2 inhibitors, including validation of inhibitor interactions with the crystallography construct and determination of the unique binding mode of 2,4-diaminopyrimidine inhibitors in the MK2 active site. Use of these tools in the optimization of a potent and selective inhibitor lead series is described in the accompanying Letter.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Maria A. Argiriadi, Anna M. Ericsson, Christopher M. Harris, David L. Banach, David W. Borhani, David J. Calderwood, Megan D. Demers, Jennifer DiMauro, Richard W. Dixon, Jennifer Hardman, Silvia Kwak, Biqin Li, John A. Mankovich, Douglas Marcotte,