A novel molecular design of thrombin receptor antagonist

被引：9

作者：

Fujita, T

Nakajima, M

Inoue, Y

Nose, T

Shimohigashi, Y ^{[1
]}

机构：

[1] Kyushu Univ, Grad Sch Sci, Dept Mol Chem, Lab Struct Funct Biochem, Fukuoka 8128581, Japan

[2] Green Cross Corp, Div Res, Hirakata, Osaka 5731153, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(99)00202-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In a computer modeling of transmembrane domains of human thrombin receptor, Lys-158 was found near the ligand binding site. To capture this basic residue, analogs of peptide ligand containing a series of acidic amino acids were synthesized and assayed for human platelet aggregation, and Ser-(p-F)Phe-Aad(= alpha-aminoadipic acid)-Leu-Arg-Asn-Pro-NH2 was found to be a potent antagonist. (C) 1999 Elsevier Science Ltd. All rights reserved.

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页码：1351 / 1356

页数：6

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