Peer-Reviewed Publication
Cancer Discov2026;16(5):953-975.May 1, 2026Journal Article
A Covalent Allosteric Molecular Glue Suppresses NRF2-Dependent Cancer Growth.
Nilotpal Roy1, Tine Wyseure1, I-Chung Lo2, Justine Lu1, Christie L Eissler1, Steffen M Bernard1, Ilah Bok3, Aaron N Snead1, Albert Parker1, U-Ging Lo1, Jason C Green1, Jordon Inloes1, Sarah R Jacinto1, Brent Kuenzi1, Marie Pariollaud1, Kathleen Negri1, Khoi Le1, Benjamin D Horning1, Noah Ibrahim1, Stephanie Grabow1, Harit Panda4, Dhaval P Bhatt3, Emily M Wilkerson3, Soma Saeidi3, Paul Zolkind4, Zoe Rush1, Heather N Williams1, Eric Walton1, Martha K Pastuszka1, John J Sigler1, Eileen Tran1, Kenneth Hee5, Joseph McLaughlin1, Géza Ambrus-Aikelin6, Jonathan Pollock1, Robert T Abraham7, Todd M Kinsella8, Gabriel M Simon1, Michael B Major3,4, David S Weinstein1, Matthew P Patricelli1
1Vividion Therapeutics, San Diego, California.
2Degron Therapeutics, San Diego, California.
3Department of Cell Biology and Physiology, Washington University School of Medicine, St. Louis, Missouri.
4Department of Otolaryngology, Washington University School of Medicine, St. Louis, Missouri.
5Sciex, Carlsbad, California.
6Genesis Therapeutics, San Diego, California.
7Engine Biosciences, Redwood City, California.
8Expedition Medicines, Cambridge, Massachusetts.
Abstract
UNLABELLED: The NRF2 transcription factor is constitutively active in cancer, in which it functions to maintain oxidative homeostasis and reprogram cellular metabolism. NRF2-active tumors exhibit NRF2 dependency and resistance to chemotherapy/radiotherapy (RT). In this study, we characterize VVD-065, a first-in-class NRF2 inhibitor that acts via an unprecedented allosteric molecular glue mechanism…
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