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J Med Chem. 1991 Jul;34(7):2068-71.

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

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  • 1Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, Illinois 60064.


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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