Determination of the core sequence of an antagonist of selectin-dependent leukocyte adhesion and correlation of its structure with molecular modeling studies

Arch Biochem Biophys. 1996 Jul 1;331(1):23-30. doi: 10.1006/abbi.1996.0278.

Abstract

The sequence 36-50 from the lectin domain of human P-selectin has been previously identified as a weak inhibitor of selectin-dependent leukocyte adhesion. A series of C- and N-terminally truncated peptides was synthesized to determine the limits of the active core region within the parent sequence. Deletions from both the N- and C-termini gave significant increases in inhibitory activity and identified 41-50 or 36-49 as minimum active sequences, but surprisingly not the common 41-49 peptide. All peptides tested showed parallel inhibition of both P- and E-selectin-dependent adhesion. A molecular model of the lectin domain was constructed using homology modeling. Examination of this model suggests one hypothesis to explain the increase in activity on deletion of Asp36.

MeSH terms

  • Amino Acid Sequence
  • Cell Adhesion / drug effects*
  • E-Selectin / chemistry*
  • Humans
  • L-Selectin / chemistry
  • Models, Molecular*
  • Molecular Sequence Data
  • Neutrophils / physiology*
  • P-Selectin / chemistry*
  • P-Selectin / pharmacology
  • Peptide Fragments / chemistry*
  • Peptide Fragments / pharmacology
  • Repetitive Sequences, Nucleic Acid

Substances

  • E-Selectin
  • P-Selectin
  • Peptide Fragments
  • L-Selectin