Treating PIK3CA and EGFR overexpressing breast cancers with lithium citrate.

摘要

The epidermal growth factor receptor (EGFR) is a membrane bound receptor tyrosine kinase of the ErbB/HER family. EGFR is most commonly expressed on cells of epithelial origin, however, it is found on the surface of most cells in the body. EGFR becomes activated at the cell surface by a variety of growth ligands, most notably the epidermal growth factor (EGF). EGF binding to the extracellular domain of EGFR causes a conformational change that exposes EGFR's dimerization domain. This conformational change allows EGFR to homo- or hetero-dimer-ize with other receptor tyrosine kinases, leading to activation of EGFR's intrinsic kinase activity and auto-phosphorylation of tyrosine residues on its C-terminal tail. These phosphorylation events allow for the association of various adaptor proteins, ultimately resulting in the activation of signaling pathways that result in cellular proliferation, migration and survival.