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