A novel phosphotyrosine mimetic 4 '-carboxymethyloxy-3 '-phosphonophenylalanine (Cpp): Exploitation in the design of nonpeptide inhibitors of pp60(Src) SH2 domain

Authors
Kawahata, N Yang, MG Luke, GP Shakespeare, WC Sundaramoorthi, R Wang, YH Johnson, D Merry, T Violette, S Guan, W Bartlett, C Smith, J Hatada, M Lu, XD Dalgarno, DC Eyermann, CJ Bohacek, RS Sawyer, TK
Citation
N. Kawahata et al., A novel phosphotyrosine mimetic 4 '-carboxymethyloxy-3 '-phosphonophenylalanine (Cpp): Exploitation in the design of nonpeptide inhibitors of pp60(Src) SH2 domain, BIOORG MED, 11(17), 2001, pp. 2319-2323
Citations number
24
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
17
Year of publication
2001
Pages
2319 - 2323
Database
ISI
SICI code
0960-894X(20010903)11:17<2319:ANPM4'>2.0.ZU;2-N
Abstract
The novel phosphotyrosine (pTyr) mimetic 4 ' -carboxymethyloxy-3 ' -phospho nophenylalanine (Cpp) has been designed and incorporated into a series of n onpeptide inhibitors of the SH2 domain of pp60(c-Src) (Src) tyrosine kinase . A 2,2 Angstrom X-ray crystal structure of la bound to a mutant form of Le k SH2 domain provides insight regarding the structure-activity relationship s and supports the design concept of this new pTyr mimetic. (C) 2001 Elsevi er Science Ltd. All rights reserved.