Ligands to the integrin receptor
v
3
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
Abstract:
The vitronectin receptor v
3 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 IIb
3 (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 IIb
3 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 v
3. Numerous patent applications and issued patents have appeared throughout the last decade claiming structurally novel v
3 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 v
3.
Keywords:
v
3;
angiogenesis;
integrin;
osteoporosis;
vitronectin
Document Type: Review article
Affiliations: 1: Department of Medicinal Chemistry, Merck Research Laboratories, WP14-2, West Point, PA 19486, USA. mark_duggan@merck.com
Publication date: 2000-09-01
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