| Literature DB >> 19919896 |
Maria A Argiriadi1, 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, Kelly D Mullen, Baofu Ni, M Pietras, Ramkrishna Sadhukhan, Silvino Sousa, Medha J Tomlinson, Lu Wang, Tao Xiang, Robert V Talanian.
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. Copyright 2009 Elsevier Ltd. All rights reserved.Entities:
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Year: 2009 PMID： 19919896 DOI： 10.1016/j.bmcl.2009.10.102
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823