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

Citation
I. Vlattas et al., IDENTIFICATION OF A RECEPTOR-BINDING REGION IN THE CORE SEGMENT OF THE HUMAN ANAPHYLATOXIN C5A, Journal of medicinal chemistry, 37(17), 1994, pp. 2783-2790
Citations number
61
Categorie Soggetti
Chemistry Medicinal
ISSN journal
00222623
Volume
37
Issue
17
Year of publication
1994
Pages
2783 - 2790
Database
ISI
SICI code
0022-2623(1994)37:17<2783:IOARRI>2.0.ZU;2-F
Abstract
In order to identify regions of C5a that contribute to receptor bindin g and functional activity of the anaphylatoxin, a series of peptides w as synthesized in which core segments have been attached to C-terminal segments via native peptidic or disulfide bonds. It has been found th at residues Arg(40) and Arg(46) in the loop-3 region of the core induc e a 1000-fold increase in the affinity of the disordered C-terminal se gment of C5a. The results obtained from this work lead to the conclusi on that the loop-3 region is most likely the core binding site of C5a.