Screening for novel inhibitors of Glutathione Peroxidase 1 and 4

National Center For Advancing Translational Sciences

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Abstract

The team has produced and purified active selenocysteine-containing recombinant human GPx1 and GPx4 using a novel method. Subsequent screening of annotated and diversity libraries yielded several promising hits of both GPx1 and GPx4. The activity of the hits was reconfirmed by testing the purified powders. The chemistry team made several analogs of one of the hits, but the activity of the analogs was found to be moderate. Another screening of an annotated library containing covalent warheads also yielded a promising hit of GPx1 and GPx4. The activity of the hit with covalent warhead was reconfirmed by testing purified powder. This hit is currently undergoing more specific characterization as it seems to be unstable in solution.