Drug Discov Ther. 2015;9(3):147-155. (DOI: 10.5582/ddt.2015.01001)

Histone deacetylase inhibitors merged with protein tyrosine kinase inhibitors.

Zhou N, Xu WF, Zhang YJ


Histone deacetylases (HDACs) are a family of metal enzymes which mainly regulates the acetylation level of histone, together with histone acetyl transferases (HATs). Recently, because many HDAC inhibitors (HDACis) have entered clinical trials for both solid and liquid tumors, HDACs are recognized as one of the promising targets for cancer treatment. The current trend is that more and more HDAC inhibitors are used in combination with other antitumor agents in order to optimize their effect and toxicity. Protein tyrosine kinases (PTKs) which play important roles in cellular signal transduction pathways and regulate series of physiological and biochemical processes, are another family of hot antitumor targets. This brief review will mainly talk about several reported chimeric HDACs-PTKs inhibitors.

KEYWORDS: HDAC, PTKs, chimeric inhibitor

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