Format

Send to

Choose Destination
See comment in PubMed Commons below
Expert Opin Investig Drugs. 2000 Jun;9(6):1281-91.

alpha(v)beta(3) Integrin antagonists as inhibitors of bone resorption.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, WP14-2, West Point, PA 19486, USA.

Abstract

The alpha(v)beta(3) integrin is a non-covalent, heterodimeric, cell-surface protein that is expressed with varying density on numerous cell types, including osteoclasts, vascular smooth muscle cells, endothelial cells and a variety of tumour cells. Functionally, alpha(v)beta(3) mediates a diverse range of biological events including the adhesion of osteoclasts to bone matrix, smooth muscle cell migration and angiogenesis. Specifically, there has been significant attention focused on the preparation of inhibitors of alpha(v)beta(3) for use as inhibitors of bone resorption, in recognition of the medical need for improved prevention and treatment of osteoporosis. Herein, we summarise the pertinent chemistry and biological advances in the medicinal design and biological evaluation of peptide and small molecule alpha(v)beta(3) antagonists as inhibitors of bone resorption.

PMID:
11060743
DOI:
10.1517/13543784.9.6.1281
[Indexed for MEDLINE]
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Taylor & Francis
    Loading ...
    Support Center