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KATs off: Biomedical insights from lysine acetyltransferase inhibitors

Journal

CURRENT OPINION IN CHEMICAL BIOLOGY
Volume 72, Issue -, Pages -

Publisher

ELSEVIER SCI LTD
DOI: 10.1016/j.cbpa.2022.102255

Keywords

Acetyltransferase; p300; CBP; MYST; GCN5; PCAF

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Lysine acetyltransferase (KAT) enzymes are important in modulating chromatin structure and transcription regulation. Recent progress has been made on developing chemical probes for p300 and MYST family of KATs, which can be useful tools for basic and translational research.
Lysine acetyltransferase (KAT) enzymes including the p300, MYST, and GCN5 families play major roles in modulating the structure of chromatin and regulating transcription. Because of their dysregulation in various disease states including cancer, efforts to develop inhibitors of KATs have steadily gained mo-mentum. Here we provide an overview of recent progress on the development of high quality chemical probes of the p300 and MYST family of KATs and how they are emerging as useful tools for basic and translational investigation.

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