IDENTIFICATION AND SYNTHESIS OF A RECEPTOR-BINDING SITE OF HUMAN ANAPHYLATOXIN C5A

被引：63

作者：

KAWAI, M

QUINCY, DA

LANE, B

MOLLISON, KW

LULY, JR

CARTER, GW

机构：

[1] Pharmaceutical Products Division, Abbott Laboratories, Abbott Park

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 34卷 / 07期

关键词：

D O I：

10.1021/jm00111a022

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

C5a is a 74 amino acid polypeptide that likely plays an important role in the pathogenesis of a number of inflammatory diseases. Therefore, the discovery of a C5a antagonist is of considerable therapeutic interest. A series of peptides designed to survey various regions of the molecule was synthesized by solid-phase peptide synthesis and evaluated for receptor-binding activity with polymorphonuclear leukocyte membranes. The C-terminal octapeptide (Ac-His-Lys-Asp-Met-Gln-Leu-Gly-Arg-OH) was identified as the smallest fragment which possessed reasonable C5a receptor binding activity.

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页码：2068 / 2071

页数：4

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