Inhibitory effect of a dimerization-arm-mimetic peptide on EGF receptor activation

被引：15

作者：

Mizuguchi, Takaaki ^{[2
]}

Uchimura, Hiromasa ^{[1
]}

Kakizawa, Taeko ^{[2
]}

Kimura, Tooru ^{[2
]}

Yokoyama, Shigeyuki ^{[3
]}

Kiso, Yoshiaki ^{[2
]}

Saito, Kazuki ^{[1
,3
,4
]}

机构：

[1] Kyoto Pharmaceut Univ, Lab Prote Sci, 21st Century COE Program, Yamashina Ku, Kyoto 6078412, Japan

[2] Kyoto Pharmaceut Univ, Dept Med Chem, Ctr Frontier Res Med Sci, Yamashina Ku, Kyoto 6078412, Japan

[3] RIKEN Syst & Struct Biol Ctr, Yokohama, Kanagawa 2300045, Japan

[4] Univ Tokyo, Grad Sch Sci, Dept Biophys & Biochem, Bunkyo Ku, Tokyo 1130033, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 12期

关键词：

A431; cells; Autophosphorylation; Dimerization-arm-mimetic peptide; Dimerization inhibitor; EGF receptor; EPIDERMAL-GROWTH-FACTOR; METASTATIC COLORECTAL-CANCER; COST-EFFECTIVENESS ANALYSIS; TYROSINE KINASE INHIBITOR; CELL LUNG; MODEL; OVEREXPRESSION; ANTIBODY; IRESSA;

D O I：

10.1016/j.bmcl.2009.04.080

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A cyclic decapeptide was chemically synthesized that mimics the loop structure of a beta-hairpin arm of the EGF receptor, which is highly involved in receptor dimerization upon activation by ligand binding. This peptide was revealed to reduce dimer formation of the receptor in a detergent-solubilized extract of epidermoid carcinoma A431 cells and to inhibit receptor autophosphorylation at less than 10 mu M in the intact cells. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：3279 / 3282

页数：4

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