Screening for small molecule degraders of KDM5A & B

National Center For Advancing Translational Sciences

Investigators

Abstract

During the reporting period, the collaborative team has expanded screening beyond drug repurposing libraries and identified several novel hits that have been validated by western blotting to reduce KDM5A & B protein levels in a breast cancer cell line. Additional primary screening work was conducted, and several novel chemotypes were identified demonstrating potent, selective modulation of KDM5A & B. Current efforts include hit profiling, mechanism of action studies and expanded screening of a new, novel molecular glue library.