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Development of c5a receptor antagonists - differential loss of functional-responses

Academic Article
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Overview

authors

  • Konteatis, Z. D.
  • Siciliano, S. J.
  • Vanriper, G.
  • Molineaux, C. J.
  • Pandya, S.
  • Fischer, P.
  • Rosen, Hugh
  • Mumford, R. A.
  • Springer, M. S.

publication date

  • November 1994

journal

  • Journal of Immunology  Journal

abstract

  • C5a is a 74-amino acid glycoprotein generated on activation of the C system. The responses evoked by C5a, both in vitro and in vivo, and its association with inflammatory diseases, suggest that a receptor antagonist would be of considerable therapeutic importance. However, efforts at generating antagonists have so far been unsuccessful. Structure/activity studies of the C terminus of C5a have generated peptide analogues with nanomolar affinities, but all of these retain strong agonist properties. We now report hexapeptides of the form NMePhe-Lys-Pro-dCha-X-dArg in which increasing aromaticity at position 5 leads to a progressive loss of agonism with little change in binding affinity. The different responses induced by C5a are lost in the order: degranulation before Ca(2+)-flux before chemotaxis. We also describe the first full antagonist of C5a, because the peptide in which x = Trp is not only devoid of all agonist properties, but it inhibits C5a induced degranulation and C5a stimulated G protein activation.

subject areas

  • Amino Acid Sequence
  • Calcium
  • Cell Degranulation
  • Chemotaxis, Leukocyte
  • Complement C5a
  • Flow Cytometry
  • GTP Phosphohydrolases
  • Humans
  • Molecular Sequence Data
  • Neutrophils
  • Peptide Fragments
  • Peroxidase
  • Protein Binding
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Identity

International Standard Serial Number (ISSN)

  • 0022-1767

PubMed ID

  • 7930622
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Additional Document Info

start page

  • 4200

end page

  • 4205

volume

  • 153

issue

  • 9

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