Novel inhibitors of the alphavbeta3 integrin--lead identification strategy

David Elliot; Eleanor Henshaw; Philip A MacFaul; Andrew D Morley; Peter Newham; Keith Oldham; Ken Page; Neil Rankine; Paul Sharpe; Attilla Ting; Christine M Wood

doi:10.1016/j.bmcl.2009.06.041

Novel inhibitors of the alphavbeta3 integrin--lead identification strategy

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4832-5. doi: 10.1016/j.bmcl.2009.06.041. Epub 2009 Jun 13.

Authors

David Elliot¹, Eleanor Henshaw, Philip A MacFaul, Andrew D Morley, Peter Newham, Keith Oldham, Ken Page, Neil Rankine, Paul Sharpe, Attilla Ting, Christine M Wood

Affiliation

¹ AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK.

PMID: 19574045
DOI: 10.1016/j.bmcl.2009.06.041

Abstract

A novel approach to inhibition of the alphavbeta3 integrin is described, which uses compounds designed to generate nM potency without using the arginine binding site.

MeSH terms

Animals
Binding Sites
Computer Simulation
Drug Design
Humans
Integrin alphaVbeta3 / antagonists & inhibitors*
Integrin alphaVbeta3 / metabolism
Oligopeptides / chemistry
Rats
Small Molecule Libraries
Structure-Activity Relationship

Substances

Integrin alphaVbeta3
Oligopeptides
Small Molecule Libraries
arginyl-glycyl-aspartic acid