Division of Genetics, Department of Medicine, Brigham and Women's Hospital, Boston, MA, 02115, USA; Department of Biological Chemistry and Molecular Pharmacology, Blavatnik Institute, Harvard Medical School, Boston, MA, 02115, USA.
Division of Genetics, Department of Medicine, Brigham and Women's Hospital, Boston, MA, 02115, USA; Department of Biological Chemistry and Molecular Pharmacology, Blavatnik Institute, Harvard Medical School, Boston, MA, 02115, USA.
Curr Opin Chem Biol. 2023 Feb;72:102255. doi: 10.1016/j.cbpa.2022.102255. Epub 2022 Dec 28.
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 momentum. 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.
赖氨酸乙酰转移酶（KAT）酶包括 p300、MYST 和 GCN5 家族，在调节染色质结构和转录调控中发挥重要作用。由于它们在包括癌症在内的各种疾病状态中的失调，开发 KAT 抑制剂的努力一直在稳步推进。本文概述了开发 p300 和 MYST 家族 KAT 的高质量化学探针的最新进展，以及它们如何成为基础和转化研究的有用工具。
