Inhibitors targeting the PWWP domain-containing proteins

• Published in: European journal of medicinal chemistry Vol. 280; p. 116965
• Main Authors: Huang, Yunyuan, Li, Boyi, Wu, Zhibin, Liu, Ke, Min, Jinrong
• Format: Journal Article
• Language: English
• Published: France Elsevier Masson SAS 15-12-2024
• Subjects: Aromatic cage; Histone binding; PWWP domain; SET domain; Histone binding; Aromatic cage; PWWP domain; SET domain
• ISSN: 0223-5234; 1768-3254; 1768-3254
• DOI: 10.1016/j.ejmech.2024.116965

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.
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•PWWP-containing proteins are linked to various diseases and serve as promising targets for drug discovery.•Compounds for PWWP-containing proteins, with unclear functions, hold promise, signaling a potential new era in this field.•Analysis of compounds targeting PWWP-containing proteins may greatly advance understanding of their role in drug development.