Discovery of Novel GST Inhibitors Identified from a DNA-Encoded Library

WuXi AppTec scientists recently contributed to a study which led to the discovery and optimization of a novel series of GST inhibitors. The authors used affinity mediated DEL selection against a privileged scaffold to identify a compound with potent inhibition against SjGST and GSTM2.

SAR studies, coupled with X-ray crystallography and structural analysis, revealed that the binding mode of this inhibitor is quite different from known GSH-like compounds.