Identification of a receptor-binding region in the core segment of the human anaphylatoxin C5a.

Autor: Vlattas I; CIBA-GEIGY Corporation, Research Department, Summit, New Jersey 07901., Sytwu II, Dellureficio J, Stanton J, Braunwalder AF, Galakatos N, Kramer R, Seligmann B, Sills MA, Wasvary J
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 1994 Aug 19; Vol. 37 (17), pp. 2783-90.
DOI: 10.1021/jm00043a017
Abstrakt: 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 Arg40 and Arg46 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.
Databáze: MEDLINE