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ST7612AA1 is an orally bioavailable, thiol-based histone deacetylase (HDAC) inhibitor currently being investigated as an epigenetic therapeutic for cancer. It acts as a prodrug that is converted into an active form containing a thiol zinc-binding group (ZBG), which chelates the catalytic zinc ion essential for HDAC enzyme function. Research indicates that resistance to ST7612AA1 can be mediated by the overexpression of sulfhydryl methyltransferases METTL7A and METTL7B, which methylate and detoxify the active thiol compound. It has shown preclinical activity in various cancer cell lines, including liver and breast cancer models.
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