The HDAC inhibitor LBH589 (panobinostat) is an inhibitory modulator of aromatase gene expression.

ABSTRACT: Aromatase converts androgens to estrogens. Although third-generation aromatase inhibitors (AIs) are important drugs in hormonal therapy for breast cancer in postmenopausal women, there are concerns about the side effects associated with the estrogen deprivation achieved with AIs. Expression of aromatase in breast cancer tissue is driven by different promoters than those in noncancer tissues; thus, suppression of aromatase expression in cancer tissues through the down-regulation of breast tumor-specific promoters would reduce the side effects associated with whole-body suppression of estrogen biosynthesis by AIs. We report that histone deacetylase inhibitor LBH589 (panobinostat) is a potent inhibitor of aromatase expression (with an IC(50) value < 25 nM). LBH589 selectively suppresses human

SUBMITTER: Chen S 

PROVIDER: S-EPMC2890707 | biostudies-literature | 2010 Jun

REPOSITORIES: biostudies-literature