Identification of small molecule inhibitors and activators of cytochrome B5 reductases (CYB5Rs)

National Center For Advancing Translational Sciences

Investigators

Abstract

We have obtained recombinant sources of CYB5R1 and CYB5R3 proteins and were able to develop and miniaturize a 1536-well biochemical assay. We have initiated the high-throughput screening of internal small molecule libraries and utilizing the data for insilico-based screening of additional collections. Initial hits are being validated by biochemical assays in the collaborator’s lab. We are evaluating the implementation of relevant cell-based assays, as well as target-engagement assays, for further characterization of hits.