Frontiers in Medicinal Chemistry

Volume: 4

Recent Developments in the Field of Non Peptidic α vβ 3 Antagonists

Author(s): Barbara Cacciari, Pamela Crepaldi, Stephanie Federico and Giampiero Spalluto

Pp: 587-618 (32)

DOI: 10.2174/978160805207310904010587

* (Excluding Mailing and Handling)


The αvβ3 receptors which are members of the group of the cellular adhesion molecules (CAM), are heterodimeric transmembrane glycoprotein receptors involved in processes such as cell-cell and cell-matrix adhesion, cell migration and signalling.

Integrin αvβ3 receptor is expressed on almost cells originating from the mesenchime and seems to mediate several biological processes, including adhesion of osteoblasts to the bone matrix, migration of vascular smooth muscle cells, and angiogenesis.

Many efforts were done in the last 15 years in order to individuate inhibitors for αvβ3 receptors, due to their involvement in important pathophysiological functions. In fact, selective αvβ3 antagonists offer new therapeutic opportunities for the treatment of several human pathologies like osteoporosis, restenosis and diseases involving neovascularization such as rheumatoid arthritis, tumour induced angiogenesis and methastasis. Purpose of this account is to summarize the recent developments in the field of non peptidic αvβ3 antagonists.

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