CPTH2 is a histone acetyltransferase (HAT) inhibitor modulating the Gcn5 network where HATs act as transcriptional coactivators. Histone acetylation plays an important role in regulating the chromatin structure and is tightly regulated by two classes of enzyme, histone acetyltransferases (HAT) and histone deacetylases (HDAC). Deregulated HAT and HDAC activity plays a role in the development of a range of cancers. Consequently, inhibitors of these enzymes have potential as anticancer agents.
Chimenti, F., et al., A Novel Histone Acetyltransferase Inhibitor Modulating Gcn5 Network: Cyclopentylidene-[4-(4'-chlorophenyl)thiazol-2-yl]hydrazone. J. Med. Chem. 52, 530-536, (2009)
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