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