Cell penetrant, potent and selective HAT Tip60 inhibitor
TH1834 is a cell penetrant, potent and selective histone acetyltransferase (HAT) Tip60 inhibitor that interact with active binding pocket of Tip60. TH1834 induces apoptosis and increased unrepaired DNA damage in breast and prostate cancer cell lines but not control MCF10A cells.
Biochemical Society transactions, 44(4), 979-986 (2016-08-17)
Two opposing enzyme classes regulate fundamental elements of genome maintenance, gene regulation and metabolism, either through addition of an acetyl moiety by histone acetyltransferases (HATs) or its removal by histone de-acetyltransferases (HDAC), and are exciting targets for drug development. Importantly
Omics : a journal of integrative biology, 24(10), 581-591 (2020-09-23)
Breast cancer is often sporadic due to several factors. Among them, the deregulation of epigenetic proteins may be involved. TIP60 or KAT5 is an acetyltransferase that regulates gene transcription through the chromatin structure. This pleiotropic protein acts in several cellular
Histone acetylation is required for many aspects of gene regulation, genome maintenance and metabolism and dysfunctional acetylation is implicated in numerous diseases, including cancer. Acetylation is regulated by histone acetyltransferases (HATs) and histone deacetylases and currently, few general HAT inhibitors
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