Minimal structural requirements for agonist activity of PAR-2 activating peptides

Bioorg Med Chem Lett. 2002 Jan 7;12(1):21-4. doi: 10.1016/s0960-894x(01)00636-9.

Abstract

Protease-activated receptor 2 (PAR-2) is involved in inflammatory, gastrointestinal, and vascular diseases. The aim of the present work was to elucidate the minimal structural features for PAR-2 agonist activity in short peptides. Our study resulted in the discovery of dipeptide derivatives of N(alpha)-benzoyl-Arg(NO(2))-Leu-NH(2) displaying a potency comparable to that of the full-length rat PAR-2 activating peptide (Ser-Leu-Ile-Gly-Arg-Leu-NH(2)).

MeSH terms

  • Animals
  • Aorta
  • Arginine / chemistry
  • Dipeptides / chemical synthesis
  • Dipeptides / chemistry
  • Dipeptides / pharmacology*
  • Drug Design
  • Drug Evaluation, Preclinical
  • Leucine / chemistry
  • Male
  • Molecular Structure
  • Muscle, Smooth, Vascular / drug effects
  • Rats
  • Rats, Wistar
  • Receptor, PAR-2
  • Receptors, Thrombin / agonists*
  • Structure-Activity Relationship

Substances

  • Dipeptides
  • Receptor, PAR-2
  • Receptors, Thrombin
  • Arginine
  • Leucine