Small molecule alpha(v) integrin antagonists: novel anticancer agents

Expert Opin Investig Drugs. 2000 Jun;9(6):1271-9. doi: 10.1517/13543784.9.6.1271.


The members of the integrin family are targets that potentially provide both therapeutic and diagnostic opportunities. Advances in the understanding of the signalling pathways, transcriptional regulation and the structure/function relationships of the adhesion molecules to extracellular matrix proteins have all contributed to these opportunities. The role of the integrins in pathological processes in both acute and chronic diseases, include ocular, cancer (solid tumours and metastasis), cardiovascular (stroke and heart failure) and inflammatory (rheumatoid arthritis) conditions. Various therapeutic candidates, including antibodies, cyclic peptides and peptidomimetics, have been identified. This review will focus on the key role of the alpha(v) integrin (alpha(v)beta(3) and alpha(v)beta(5)) in angiogenic processes in tumours, including its potential use in cancer diagnostics and therapy.

Publication types

  • Review

MeSH terms

  • Angiogenesis Inhibitors / pharmacology*
  • Animals
  • Antineoplastic Agents / pharmacology*
  • Humans
  • Integrins / antagonists & inhibitors*
  • Ligands
  • Receptors, Vitronectin / antagonists & inhibitors*


  • Angiogenesis Inhibitors
  • Antineoplastic Agents
  • Integrins
  • Ligands
  • Receptors, Vitronectin
  • integrin alphaVbeta5