Carbacyclic peptide mimetics as VCAM-VLA-4 antagonists

Bioorg Med Chem Lett. 2000 Jun 5;10(11):1163-5. doi: 10.1016/s0960-894x(00)00173-6.

Abstract

Substitution of carbon for sulfur in a potent 13-membered cyclic disulfide containing peptide was accomplished via an intramolecular Wittig reaction and resulted in a series of 'carba' analogues. Potency in the VCAM-VLA-4 assay was sensitive to ring size and lower than that of the parent disulfide.

MeSH terms

  • Integrin alpha4beta1
  • Integrins / antagonists & inhibitors*
  • Molecular Mimicry
  • Peptides, Cyclic / chemistry
  • Peptides, Cyclic / pharmacology*
  • Receptors, Lymphocyte Homing / antagonists & inhibitors*
  • Vascular Cell Adhesion Molecule-1 / drug effects*

Substances

  • Integrin alpha4beta1
  • Integrins
  • Peptides, Cyclic
  • Receptors, Lymphocyte Homing
  • Vascular Cell Adhesion Molecule-1