EGFR

Epidermal growth factor receptor (EGFR), also known as ERBB, HER1, mENA, ERBB1, PIG61, and NISBD2, belongs to the protein kinase (Tyr protein kinase) superfamily and it contains one protein kinase domain in its protein sequence. EGFR is a transmembrane protein with the N terminal region exposed at the cell surface for ligand binding. Known ligands of EGFR include EGF, TGFAa, amphiregulin, epigen, betacellulin, epiregulin, and heparin-binding EGF. Upon ligand binding, EGFR forms homodimer with an adjacent EGFR or heterodimer with another receptor in the EGFR superfamily and activates the downstream cellular signaling cascades (RAS-RAF-MEK-ERK, PI3 kinase-AKT, PLCgamma-PKC and STATs modules) and induces cell proliferation.

Abnormal EGFR expression or EGFR overexpression is associated with various disorders including squamous-cell carcinoma of the lung, anal cancers, glioblastoma, and epithelian tumors of the head and neck. It is also related to several inflammatory diseases and monogenic diseases. The overexpression of EGFR in tumor cells makes it an appealing target for immunotherapies, especially ADCs due to the observed internalization of the EGFR upon ligand binding.

Entrez Gene ID: 1956
UniProt ID: P00533