Overcoming EGFR resistance by monovalent and bident inhibitors targeting Cys775
Zhengnian Li, Jie Jiang, Yaning Wang, Scott B. Ficarro, Stephen J. Collins, Tyler S. Beyett, Ilse K. Schaeffner, Isidoro Tavares, Felix H. Gottlieb, Dhiraj Suda, Prafulla C. Gokhale, Leah M. Black-Holmes, Dimitris Gazgalis, Michael J. Eck, Pasi Antero Janne, , Tinghu Zhang
This paper develops covalent EGFR inhibitors targeting cysteine 775 and 797, showing improved efficacy and resistance delay in osimertinib-resistant models.
ACS Central Science · Sep 29, 2026Peer-reviewedCancer Biology