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A two-faced selectivity solution to target SMARCA2 for cancer therapy

Two new studies exploring PROTAC-mediated degradation of SMARCA2 for cancer therapy solve an apparently intractable selectivity challenge with SMARCA4 by utilising the requirement for a productive ternary complex between the protein, PROTAC and ligase complex.

Detalles Bibliográficos
Autores principales: Harling, John D., Tinworth, Christopher P.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9889305/
https://www.ncbi.nlm.nih.gov/pubmed/36720862
http://dx.doi.org/10.1038/s41467-023-36238-0
Descripción
Sumario:Two new studies exploring PROTAC-mediated degradation of SMARCA2 for cancer therapy solve an apparently intractable selectivity challenge with SMARCA4 by utilising the requirement for a productive ternary complex between the protein, PROTAC and ligase complex.