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.
Vividion's march towards a covalent WRN inhibitor and one of the first to clinic. Interestingly, they took an ATP-competitive compound and converted it into an ATP-cooperative analogue. Finally out in Nature. https://t.co/c2VzFfGiqG
Nature research paper: Discovery of WRN inhibitor HRO761 with synthetic lethality in MSI cancers https://t.co/o8ZC2IIcvM
Delighted to see this work on the first inhibitor/degrader of the Werner Helicase (WRN), finally published. A genetically defined synthetic lethality, to be tested in the human model system of disease. Congratulations to all from NIBR who led this program. https://t.co/ldQWc6FTw2
@VividionRx Chemoproteomic discovery of a covalent allosteric inhibitor of WRN helicase | Nature https://t.co/iA5z1urEqd
Nature research paper: Chemoproteomic discovery of a covalent allosteric inhibitor of WRN helicase https://t.co/0vmWwkObT1
"Discovery of WRN inhibitor HRO761 with synthetic lethality in MSI cancers" https://t.co/tx1Z5qXyjg