High-throughput screening for inhibitors of metabolic checkpoints on the G2/mitosis transition

National Center For Advancing Translational Sciences

Investigators

Abstract

One fundamental question in cancer biology is how cancer cells sense metabolic status (often reflected by the level of key intermediate metabolites), and in turn adapt to changes of metabolic status and sustain cell proliferation. The mechanisms of metabolic checkpoints are poorly understood. This project aims to use chemical library screening to identify small molecules that can restore G2/M phase transition, and in turn identify their biological targets. During this reporting period, a cell-based HTS amenable assay was developed and focused library screening was conducted. Hit molecules were cherry-picked and tested in a panel of confirmatory assays, and bioinformatics approaches are currently underway to help identify and validate the biological targets of active compounds.