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HER2, also known as ErbB-2 or ERBB2, is a member of the ErbB family of receptor tyrosine kinases. It is a transmembrane glycoprotein that acts as a preferred dimerization partner for other ErbB family members, leading to autophosphorylation and activation of downstream signaling pathways such as MAPK/ERK and PI3K/Akt. Overexpression or amplification of HER2 is found in various cancers, particularly breast and gastric cancers, driving uncontrolled cell proliferation and correlating with poor prognosis. Therapeutic strategies targeting HER2 include monoclonal antibodies, antibody-drug conjugates, and small molecule kinase inhibitors.
Monoclonal antibodies bind to the extracellular domain of HER2, inhibiting dimerization and downstream signaling. Antibody-drug conjugates deliver cytotoxic drugs to HER2-expressing cells. Small molecule kinase inhibitors block the intracellular tyrosine kinase activity of HER2.
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