Disrupting aberrant EGFR catalytic trimers reverses T790M gefitinib resistance
Epidermal growth factor receptor (EGFR) mutations drive up to 50% of non-small-cell lung cancers (NSCLC). Although tyrosine kinase inhibitors provide substantial clinical benefit, remissions are prematurely terminated by the inevitable acquisition of on-target resistance. Beyond structural changes that alter ATP-pocket affinity, EGFR oligomerization drives this resistance, though the underlying…
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