Trichostatin A (TSA), is an antifungal antibiotic. It’s cytostatic and differentiating properties are utilized in mammalian cell culture. It is a potent and specific, nonselective HDAC inhibitor, shown to have anti-inflammatory and neuroprotective properties. It inhibits all class I and class II HDAC’s and induces histone acetylation. TSA interacts reversibly with the HDAC catalytic site preventing binding of the substrate. HDACs - Classes I, II, and IV all require a zinc molecule as an essential cofactor in their active site and are inhibited by Zn2+-binding HDAC inhibitor - Trichostatin A?(TSA).?
Studies have shown antiproliferative and HDAC inhibitory activity of TSA in vitro, in human breast cancer cell lines. its antitumor efficacy and toxicity has been studied in vivo in a carcinogen-induced rat mammary cancer model, which provided evidence for potent dose-dependent antitumor activity of TSA against breast cancer in vitro and in vivo. These studies strongly support HDAC as a molecular target for anticancer therapy in breast cancer.
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