IDENTIFICATION OF A RECEPTOR-BINDING REGION IN THE CORE SEGMENT OF THE HUMAN ANAPHYLATOXIN C5A

被引:10
作者
VLATTAS, I
SYTWU, II
DELLUREFICIO, J
STANTON, J
BRAUNWALDER, AF
GALAKATOS, N
KRAMER, R
SELIGMANN, B
SILLS, MA
WASVARY, J
机构
[1] CIBA-GEIGY Corporation, Pharmaceuticals Division, Research Department, Summit
[2] Selectide Corporation, Tucson, AZ 85737, 10900 N. Stallard Place
关键词
D O I
10.1021/jm00043a017
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In order to identify regions of C5a that contribute to receptor binding and functional activity of the anaphylatoxin, a series of peptides was synthesized in which core segments have been attached to C-terminal segments via native peptidic or disulfide bonds. It has been found that residues Arg(40) and Arg(46) in the loop-3 region of the core induce a 1000-fold increase in the affinity of the disordered C-terminal segment of C5a. The results obtained from this work lead to the conclusion that the loop-3 region is most likely the core binding site of C5a.
引用
收藏
页码:2783 / 2790
页数:8
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