Novel phosphotyrosine mimetics in the design of peptide ligands for pp60(src) SH2 domain

被引：27

作者：

Shahripour, A

Plummer, MS

Lunney, EA

Para, KS

Stankovic, CJ

Rubin, JR

Humblet, C

Fergus, JH

Marks, JS

Herrera, R

Hubbell, SE

Saltiel, AR

Sawyer, TK

机构：

[1] WARNER LAMBERT PARKE DAVIS, PARKE DAVIS PHARMACEUT RES, DEPT BIOCHEM, ANN ARBOR, MI 48105 USA

[2] WARNER LAMBERT PARKE DAVIS, PARKE DAVIS PHARMACEUT RES, DEPT SIGNAL TRANSDUCT, ANN ARBOR, MI 48105 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 11期

关键词：

D O I：

10.1016/0960-894X(96)00208-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have designed and synthesized a series of phosphorylated penta- and tri-peptides of general structures R-x-Glu-Glu-Ile-Glu and R-x-Glu-D-Trp-NH2, where R-x represents a phosphotyrosine mimetic. These peptides show binding affinity to pp60(src) SH2 domain in the micromolar range. Data are presented that provide an account of their structure-activity relationships and specificity properties. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：1209 / 1214

页数：6

共 19 条

[1]

BHATTACHARYA KK, 1980, INDIAN J CHEM B, V19, P191

[2] NONHYDROLYZABLE PHOSPHOTYROSYL MIMETICS FOR THE PREPARATION OF PHOSPHATASE-RESISTANT SH2 DOMAIN INHIBITORS [J].