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
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
收藏
页码:3279 / 3282
页数:4
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