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ID: ALA1125281

Journal: J Med Chem

Title: Identification and synthesis of a receptor binding site of human anaphylatoxin C5a.

Authors: Kawai M, Quincy DA, Lane B, Mollison KW, Luly JR, Carter GW.

Abstract: 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.

CiteXplore: 2066977

DOI: 10.1021/jm00111a022