The Constrained Amino Acid β‐Acc Confers Potency and Selectivity to Integrin Ligands

Abstract

Complete opposites: The incorporation of the rigid building block (+)-β-Acc (Acc=aminocyclopropane carboxylic acid) into cyclic RGD peptides results in a high affinity towards the integrin αvβ3. The peptides 1 and 2 are composed of the enantiomeric building blocks (+)- (blue) and (−)-β-Acc (red). The active peptide 1 inhibits integrin αvβ3 mediated cell adhesion to vitronectin with an IC50 value of 20 nM. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2007/z605248_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.