ChemInform Abstract: Combinatorial Chemistry Techniques Applied to Nonpeptide Integrin Antagonists

Autor:	W. J. Hoekstra, B. L. Poulter
Rok vydání:	2010
Předmět:	biology Combinatorial Chemistry Techniques Chemistry Integrin General Medicine Pharmacology Combinatorial chemistry Fibronectin Extracellular matrix Cell surface receptor Antithrombotic biology.protein Vitronectin Cell adhesion
Zdroj:	ChemInform. 29
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.199834317
Popis:	The integrins are cell surface receptors that recognize extracellular matrix adhesive proteins such as fibrinogen, fibronectin, vitronectin, and VCAM-1 (vascular cell adhesion molecule-1). Nonpeptide integrin antagonists designed after the adhesion recognition sequence RGD (Arg-Gly-Asp) not only have displayed efficacy as antithrombotic agents, but also have promise for the treatment of cancer and osteoporosis. Combinatorial organic syntheses of chemical mini-libraries have facilitated nonpeptide lead optimization of integrin antagonists with marked success. Although these accomplishments have been realized primarily for the discovery of orally active GPIIb/IIIa antagonist antithrombotics, vitronectin receptor (avb3) antagonist research has also benefited from such rapid synthesis. The purpose of this review is to report progress in combinatorial synthesis lead optimization by highlighting the drug design strategies and synthetic tactics that have led to improved integrin antagonists.
Databáze:	OpenAIRE
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