Revisiting the molecular mechanism of acquired resistance to reversible tyrosine kinase inhibitors caused by EGFR gatekeeper T790M mutation in non-small-cell lung cancer

ConclusionEAI045, the first fourth-generation EGFR inhibitor, exhibits a moderate affinity to EGFR andpossesses an exquisite selectivity for wild type over mutant kinase (~3-fold). This is expected if consideringthat the EAI045 is an allosteric inhibitor, which does not need to directly compete with ATP, and high affinityand selectivity are therefore not required for the inhibitor.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research