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Non Peptidic αvβ3 Antagonists: Recent Developments

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The αvβ3 receptor, 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 signaling. Integrin αvβ3 receptor is expressed on almost all cells originating from the mesenchyme and seem 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 10 years 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, tumor induced angiogenesis and metastasis. Purpose of this account is to summarize the recent developments in the field of non-peptidic αvβ3 antagonists.

Keywords: carcinoma; cellular adhesion molecules; crystal structure; integrins; osteoblasts; vitronectin receptor

Document Type: Review Article


Affiliations: Dipartimento di Scienze Farmaceutiche, Piazzale Europa 1, I-34127 Trieste, Italy.

Publication date: 2005-01-01

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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