qHTS to Identify Activators and Inhibitors of Wip1

National Center For Advancing Translational Sciences

Investigators

Abstract

During this period, the project team ordered and purified commercially available powders of HTS hits that consisted of both inhibitors and activators of WIP1. We identified one activator and two inhibitors, one competitive and one uncompetitive; these confirmed activity in the the RapidFire mass spectrometry screening assay, the fluorescence reporter orthogonal assay, and binding studies by surface plasmon resonance (SPR). These new scaffolds could be candidates for optimization which may lead to inhibitors with better pharmacokinetics and to the first-in-class WIP1 activator.