Xuejiao Shirley Guo, Abdalrahman Khalifa, Karthik Selvam, Tatiana G Kutateladze, Wenshe Ray Liu
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引用次数: 0
Abstract
The YEATS domain is an evolutionarily conserved epigenetic reader that specifically recognizes post-translational lysine acylation on histone tails and plays a crucial role in chromatin remodeling and transcriptional regulation. Four human YEATS domain-containing proteins, ENL, AF9, YEATS2, and GAS41, have been implicated in the pathogenesis of various malignancies. This review provides an overview of the structural basis for the YEATS domain's recognition of diverse acyllysine post-translational modifications and discusses the disease-related consequences of aberrant YEATS activity. Emphasis is placed on recent progress in the development of chemical modulators, including peptide-based inhibitors, small molecules, and proteolysis-targeting chimeras (PROTACs), that represent promising strategies for the selective targeting of YEATS domains. These developments underscore the potential of YEATS-directed therapies in epigenetic drug discovery.
期刊介绍：
ACS Chemical Biology provides an international forum for the rapid communication of research that broadly embraces the interface between chemistry and biology.
The journal also serves as a forum to facilitate the communication between biologists and chemists that will translate into new research opportunities and discoveries. Results will be published in which molecular reasoning has been used to probe questions through in vitro investigations, cell biological methods, or organismic studies.
We welcome mechanistic studies on proteins, nucleic acids, sugars, lipids, and nonbiological polymers. The journal serves a large scientific community, exploring cellular function from both chemical and biological perspectives. It is understood that submitted work is based upon original results and has not been published previously.
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