Vitronectin receptor alpha(V)beta(3) integrin antagonists: chemical and structural requirements for activity and selectivity

Mini Rev Med Chem. 2002 Dec;2(6):531-42. doi: 10.2174/1389557023405602.

Abstract

Alpha(V)beta(3) integrin, a cell surface protein, has been targeted by a variety of natural and synthetic antagonists in the search for potential cancer and osteoporosis drug candidates. This review discusses chemical and structural requirements for activity and selectivity deduced from SAR studies and draws a tentative picture of the pharmacophore.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Benzodiazepines / chemistry
  • Benzodiazepines / pharmacology*
  • Drug Design*
  • Integrin alphaVbeta3 / antagonists & inhibitors*
  • Peptides, Cyclic / chemistry
  • Peptides, Cyclic / pharmacology*
  • Structure-Activity Relationship

Substances

  • Integrin alphaVbeta3
  • Peptides, Cyclic
  • Benzodiazepines