Vitronectin Receptor -αVβ3 Integrin- Antagonists: Chemical and Structural Requirements for Activity and Selectivity

Christophe      Henry; Nicolas      Moitessier; Yves      Chapleur

doi:10.2174/1389557023405602

Abstract

αVβ3 integrin, a cell surface protein, has been targeted by a variety of natural and synthetic antagonists in the search for potential cancer and osteoporosis drug candidates. This review discusses chemical and structural requirements for activity and selectivity deduced from SAR studies and draws a tentative picture of the pharmacophore.

Keywords: vitronectin receptor, activity and selectivity, cell surface protein, antagonists, heterodimeric non-covalent proteins, tumour metastasis, thrombotic disorder treatment, snake venom proteins, pseudo-peptides, pseudo-peptidic antagonists

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Mini-Reviews in Medicinal Chemistry

Title: Vitronectin Receptor -αVβ3 Integrin- Antagonists: Chemical and Structural Requirements for Activity and Selectivity

Volume: 2 Issue: 6

Author(s): Christophe Henry, Nicolas Moitessier and Yves Chapleur

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Abstract: αVβ3 integrin, a cell surface protein, has been targeted by a variety of natural and synthetic antagonists in the search for potential cancer and osteoporosis drug candidates. This review discusses chemical and structural requirements for activity and selectivity deduced from SAR studies and draws a tentative picture of the pharmacophore.

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Henry Christophe, Moitessier Nicolas and Chapleur Yves, Vitronectin Receptor -αVβ3 Integrin- Antagonists: Chemical and Structural Requirements for Activity and Selectivity, Mini-Reviews in Medicinal Chemistry 2002; 2 (6) . https://dx.doi.org/10.2174/1389557023405602