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Design, Synthesis, and Biological Evaluation of the First Novel Macrocycle-Based FGFR Inhibitors That Overcome Clinically Acquired Resistance
Abstract Click to copy section linkSection link copied! Alterations in the FGFR family act as oncogenic drivers for multiple pediatric and adult tumors, leading to the development and approval of several FGFR inhibitors. However, the on-target gatekeeper and “molecular brake” mutations confer clinically acquired resistance to the FDA-approved FGFR inhibitors, which presents a significant unmet medical need.
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