Screening for small molecule degraders of KDM5A & B

National Center For Advancing Translational Sciences

Investigators

Abstract

The NCATS Early Translation Branch (ETB) hosts a broad and comprehensive program for the discovery of drug candidates directed towards rare diseases and pharmacological tools to probe the function of the human genome. ETB conducts research to understand the underlying principles driving the translation of basic research discoveries into tangible improvements in human health. During the reporting period, the collaborative team has completed screening of drug repurposing libraries and identified several 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 validation and profiling.