The paper develops covalent ligands that specifically target a complexoform of TRMT112, revealing partner-specific functional effects through allosteric activation of METTL5.

Nature Chemical Biology · Jan 8, 2026Peer-reviewedBiochemistry

Suppression of NRF2-dependent cancer growth by a covalent allosteric molecular glue

Nilotpal Roy, Tine L Wyseure, I‐Chung Lo, Justine Lu, Christie L. Eissler, Steffen M. Bernard, Ilah Bok, Aaron Nathan Snead, Aulma R. Parker, U‐Ging Lo, Jason C. Green, Jordon M. Inloes, Sarah R. Jacinto, Brent M. Kuenzi, Marie Pariollaud, , Matthew P. Patricelli

This paper introduces VVD-065, a covalent NRF2 inhibitor that enhances NRF2 degradation and sensitizes tumors to therapy, supporting a Phase I clinical trial.

Cancer Discovery · Dec 19, 2025Peer-reviewedCancer Biology

Covalent inhibitors of the RAS binding domain of PI3Ka impair tumor growth driven by RAS and HER2

Joseph E. Klebba, Nilotpal Roy, Steffen M. Bernard, Stephanie Grabow, Melissa A. Hoffman, Hui Miao, Junko Tamiya, Jinwei Wang, Cynthia Berry, Antonio Esparza-Oros, Richard D. Lin, Yongsheng Liu, Marie Pariollaud, Holly Parker, Igor Mochalkin, , Matthew P. Patricelli

The paper develops covalent inhibitors targeting the RAS binding domain of PI3Kα, showing efficacy against RAS and HER2-driven tumors without affecting glucose homeostasis.

Science · Oct 9, 2025Peer-reviewedCancer Biology