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Inhibition of angiogenesis by the antifungal drug itraconazole.

Abstract：

:Angiogenesis, the formation of new blood vessels, is implicated in a number of important human diseases, including cancer, diabetic retinopathy, and rheumatoid arthritis. To identify clinically useful angiogenesis inhibitors, we assembled and screened a library of mostly Food and Drug Administration-approved drugs for inhibitors of human endothelial cell proliferation. One of the most promising and unexpected hits was itraconazole, a known antifungal drug. Itraconazole inhibits endothelial cell cycle progression at the G1 phase in vitro and blocks vascular endothelial growth factor/basic fibroblast growth factor-dependent angiogenesis in vivo. In attempts to delineate the mechanism of action of itraconazole, we found that human lanosterol 14alpha-demethylase (14DM) is essential for endothelial cell proliferation and may partially mediate the inhibition of endothelial cells by itraconazole. Together, these findings suggest that itraconazole has the potential to serve as an antiangiogenic drug and that lanosterol 14DM is a promising new target for discovering new angiogenesis inhibitors.

journal_name

ACS Chem Biol

journal_title

ACS chemical biology

authors

Chong CR,Xu J,Lu J,Bhat S,Sullivan DJ Jr,Liu JO

doi

10.1021/cb600362d

subject

Has Abstract

pub_date

2007-04-24 00:00:00

pages

263-70

issue

4

eissn

1554-8929

issn

1554-8937

journal_volume

2

pub_type

杂志文章

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