High-throughput screening to identify small molecule inhibitors of deoxyhypusine synthase and deoxyhypusine hydroxylase

National Center For Advancing Translational Sciences

Investigators

Abstract

This project aims to identify novel small molecules inhibitors of DHS and DOHH that may prove to be useful anticancer agents. During this period, the collaborative team has successfully developed a 384-well high-throughput DHS assay which enables the direct detection of enzymatic products Rapidfire mass spectrometry. Assay conditions and parameters such as incubation time, Km, Z' and the signal-to-background ratio have been optimized and determined to be sufficiently robust to support high-throughput screening against NCGC's small molecule collections.