qHTS to Identify Activators and Inhibitors of Wip1

National Center For Advancing Translational Sciences

Investigators

Abstract

The NCATS Early Translation Branch (ETB) hosts a broad and comprehensive program for the discovery of drug candidates directed towards rare diseases and pharmacological tools to probe the function of the human genome. ETB conducts research to understand the underlying principles driving the translation of basic research discoveries into tangible improvements in human health. During this period, the project team worked to validate previously identified inhibitors and activators of WIP1. The team confirmed activity of these molecules in a RapidFire mass spectrometry screening assay, fluorescence reporter orthogonal assay, and binding studies by surface plasmon resonance (SPR). These new scaffolds could be candidates for optimization, which may provide better pharmacokinetics. Chemistry team in Dr. Appella's lab continued on lead optimization to generate SAR data for the lead series and tested the activity in MS assay at NCATS.