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.
MeSH terms
-
Amino Acid Sequence
-
Binding Sites
-
Binding, Competitive / drug effects
-
Cell Membrane / drug effects
-
Cell Membrane / metabolism
-
Complement C5a / antagonists & inhibitors
-
Complement C5a / metabolism*
-
Humans
-
Molecular Sequence Data
-
Neutrophils / drug effects
-
Neutrophils / metabolism
-
Oligopeptides / chemical synthesis*
-
Oligopeptides / pharmacology
-
Peptide Fragments / chemical synthesis*
-
Peptide Fragments / pharmacology
-
Receptors, Complement / drug effects
-
Receptors, Complement / metabolism*
Substances
-
Oligopeptides
-
Peptide Fragments
-
Receptors, Complement
-
acetylhistidyl-lysyl-aspartyl-methionyl-glutaminyl-leucyl-glycyl-arginine
-
Complement C5a