Dirigir la proteína 2 del dominio SET que se une al receptor nuclear (NSD2) para la terapia del cáncer: Desafíos y...

The nuclear receptor-binding SET domain protein NSD2 plays a crucial role in the pathogenesis and progression of various tumors. In recent years, NSD2 has garnered widespread attention as a potential therapeutic target for tumor-related diseases-with NSD2 inhibitors and degraders emerging as key research focuses in this field. Although several NSD2 inhibitors and degraders have been identified, most remain in the early stages of drug development. This review provides a comprehensive and systematic exploration of NSD2 inhibitors and degraders in the context of tumor therapy. Specifically, these small molecules are classified and elaborated based on their structural characteristics; for each structural category, the binding modes, structural features, and pharmacological activities of typical compounds are analyzed in detail, while their inherent advantages and limitations are critically evaluated. Collectively, this review offers valuable insights and guidance for the future research and development of safer, more effective, and more targeted NSD2 small-molecule agents.