1skj

From Proteopedia

Revision as of 00:19, 21 November 2007

COCRYSTAL STRUCTURE OF UREA-SUBSTITUTED PHOSPHOPEPTIDE COMPLEX

Overview

The specific association of an SH2 domain with a phosphotyrosine, (pTyr)-containing sequence of another protein precipitates a cascade of, intracellular molecular interactions (signals) which effect a wide range, of intracellular processes. The nonreceptor tyrosine kinase Src, which has, been associated with breast cancer and osteoporosis, contains an SH2, domain. Inhibition of Src SH2-phosphoprotein interactions by small, molecules will aid biological proof-of-concept studies which may lead to, the development of novel therapeutic agents. Structure-based design, efforts have focused on reducing the size and charge of Src SH2 ligands, while increasing their ability to penetrate cells and reach the, intracellular Src SH2 domain target. In this report we describe the, synthesis, binding affinity, and Src SH2 cocrystal structure of a small, novel, nonpeptide, urea-containing SH2 domain ligand.

About this Structure

1SKJ is a Single protein structure of sequence from Rous sarcoma virus with UR2 as ligand. Active as Transferase, with EC number and 2.7.10.2 2.7.10.1 and 2.7.10.2 Full crystallographic information is available from OCA.

Reference

Design, synthesis, and cocrystal structure of a nonpeptide Src SH2 domain ligand., Plummer MS, Holland DR, Shahripour A, Lunney EA, Fergus JH, Marks JS, McConnell P, Mueller WT, Sawyer TK, J Med Chem. 1997 Nov 7;40(23):3719-25. PMID:9371236

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