Anti-angiogenesis is a promising strategy for the treatment of
cancer.
Integrins, consisting of two noncovalently bound transmembrane alpha and beta subunits, are an important molecular family involved in
tumor angiogenesis. The blockade of
integrin signaling has been demonstrated to be efficient to inhibit
tumor growth, angiogenesis, and
metastasis. Among all the
integrins, alpha(v)beta(3) seems to be the most important one during
tumor angiogenesis. The inhibition of
integrin alpha(v)beta(3) signaling with
antibodies,
peptides,
peptidomimetics, and other antagonists has great potential in the treatment of
cancer. In addition,
integrin alpha(v)beta(3) is highly expressed on activated endothelial cells, new-born vessels as well as some
tumor cells, but is not present in resting endothelial cells and most normal organ systems, making it a suitable target for anti-angiogenic
therapy. In this article we will review the role of
integrin alpha(v)beta(3) in angiogenesis, present recent progress in the use of
integrin alpha(v)beta(3) antagonists and
integrin-targeted delivery systems as potential
cancer therapeutics, and discuss future perspectives.