[HTML][HTML] Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein
Aberrant signaling of ErbB family members human epidermal growth factor 2 (HER2) and
epidermal growth factor receptor (EGFR) is implicated in many human cancers, and HER2
expression is predictive of human disease recurrence and prognosis. Small molecule kinase
inhibitors of EGFR and of both HER2 and EGFR have received approval for the treatment of
cancer. We present the first high resolution crystal structure of the kinase domain of HER2 in
complex with a selective inhibitor to understand protein activation, inhibition, and function at …
epidermal growth factor receptor (EGFR) is implicated in many human cancers, and HER2
expression is predictive of human disease recurrence and prognosis. Small molecule kinase
inhibitors of EGFR and of both HER2 and EGFR have received approval for the treatment of
cancer. We present the first high resolution crystal structure of the kinase domain of HER2 in
complex with a selective inhibitor to understand protein activation, inhibition, and function at …