Breakthrough WRN Inhibitor HRO761 Targets MSI Cancers, Poised for Clinical Trials

Apr 24, 2024, 07:56 PM

Recent research has led to the discovery of a novel inhibitor, HRO761, targeting Werner Helicase (WRN), which shows synthetic lethality in microsatellite instability (MSI) cancers. This breakthrough, published in Nature, was achieved through chemoproteomic techniques that identified a covalent allosteric inhibitor of WRN. The research, spearheaded by NIBR and involving Vividion, marks a significant advancement in cancer treatment, particularly by transforming an ATP-competitive compound into an ATP-cooperative analogue. The development is poised for clinical testing to evaluate its effectiveness in human models of disease.