https://www.danafarberplga.org/wp-content/uploads/2014/04/2.jpg 1429 1302 Tam /wp-content/uploads/2020/04/PLGA-DFCI-logo-left-title-right-v6.jpg Tam2014-12-01 14:28:552014-12-01 14:28:55Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors
Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors
In this month’s featured publication, researchers in Dr. Gray’s group expand upon previous studies of the FGFR receptor, a protein found mutated in a subset of pilocytic astrocytomas. However, a common problem in cancer is development of tumor resistance to chemotherapy over time. Using structure-based drug design, they developed two next-generation covalent inhibitors that can overcome the most common form of resistance, a mutation of the FGFR itself, called the gate-keeeper mutation. These new inhibitors prevented the actions of FGFR on cultured cells, and will serve as prototype inhibitors that will undergo further preclinical validation.