Ligands to the integrin receptor v3
Authors: Duggan M.E.; Hutchinson J.H.
Source: Expert Opinion on Therapeutic Patents, Volume 10, Number 9, September 2000 , pp. 1367-1383(17)
Publisher: Informa Healthcare
The vitronectin receptor v3 is a member of the integrin superfamily of membrane bound glycoprotein receptors that is responsible for cell-cell and cell-matrix interactions and shares the same subunit as the fibrinogen receptor IIb3 (also known as GPIIb/IIIa). Both these integrins recognise extracellular proteins that express the peptide sequence arginine-glycine-aspartic acid (RGD). Non-peptide RGD mimetics that bind with high affinity and selectivity to IIb3 were previously prepared as anti-thrombotic agents. More recently, medicinal chemistry groups have modified these non-peptide fibrinogen receptor antagonist lead structures to impart potency and integrin selectivity for v3. Numerous patent applications and issued patents have appeared throughout the last decade claiming structurally novel v3 antagonists as agents for the prevention and/or treatment of osteoporosis, cancer, diabetic retinopathy and rheumatoid arthritis. This review encompasses those issued patents and published patent applications that disclose ligands to v3.
Document Type: Review article
Publication date: 2000-09-01