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.