KATs off：来自赖氨酸乙酰转移酶抑制剂的生物医学见解。
KATs off: Biomedical insights from lysine acetyltransferase inhibitors.
发表日期：2023 Feb
作者：
Samuel D Whedon, Philip A Cole
来源：
CURRENT OPINION IN CHEMICAL BIOLOGY
摘要：
Lysine乙酰转移酶（KAT）酶，包括p300，MYST和GCN5家族，在调节染色质结构和调控基因转录中发挥重要作用。由于它们在包括癌症在内的各种疾病状态下的失调，开发KAT抑制剂的努力不断获得动力。在这里，我们概述了关于p300和MYST家族KAT的高质量化学探针研发的最新进展，并介绍它们如何成为基础和转化研究的有用工具。 版权所有©2022 Elsevier Ltd。保留所有权利。
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.Copyright © 2022 Elsevier Ltd. All rights reserved.