Inhibitors targeting the PWWP domain-containing proteins.

PWWP domain-containing proteins play a pivotal role in chromatin-mediated biological processes, and their aberrant regulation is linked to various human diseases. Recent years have witnessed remarkable strides in unraveling the structural and functional features of PWWP domain-containing proteins, propelling significant advances in targeting the PWWP domain-containing proteins for drug discovery purposes. Several drugs have already been approved, while others are currently in clinical trials. This review offers a comprehensive overview of the latest developments on PWWP domain-containing proteins, including their structural characteristics and biological significance. It also provides detailed insights into the drug discovery process targeting these proteins, including screening, design, and structural optimization. Copyright © 2024 Elsevier Masson SAS. All rights reserved.

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Yunyuan Huang, Boyi Li, Zhibin Wu, Ke Liu, Jinrong Min. Inhibitors targeting the PWWP domain-containing proteins. European journal of medicinal chemistry. 2024 Dec 15;280:116965

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PMID: 39413441

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