Description
General description
Epidermal growth factor receptor (EGFR) can be activated by binding EGF or at least six other structurally related protein ligands, including transforming growth factor-α (TGF-α), heparin-binding EGF-like growth factor (HB-EGF), betacellulin (BTC), amphiregulin, epiregulin and epigen. Human EGFR T790M L858R (GenBank Accession No. NM_005228), (amino acids 668-1210) with N-terminal GST tag, MW = 88kDa, expressed in baculovirus expression system.
The EGFR gene is mapped to human chromosome 7p11.2 and encodes a 170 kDa receptor protein belonging to the HER (Receptor tyrosine-protein kinase erbB-4) family of receptor tyrosine kinases. Egfr is localized to epithelial cell surface.
Application
Useful for the study of enzyme kinetics, screening inhibitors, and selectivity profiling.
Biochem/physiol Actions
Epidermal growth factor receptor (EGFR, ErbB1) is a transmembrane protein that exerts tyrosine kinase activity upon ligand induced activation. The receptor undergoes dimerization and phosphorylation of tyrosine kinase. Upon activation by ligands, epidermal growth factor receptor (EGFR, ErbB1) initiates a signaling cascade which includes dimerization and internalization, tyrosine phosphorylation, DNA synthesis of target genes, and, ultimately, cell proliferation. EGFR signaling plays a role in the growth and differentiation of normal cells, but elevated EGFR activity is correlated with the development and pathogenesis of certain cancers. Mutation in the EGFR gene is associated with the risk of tumor development including glioma, colorectal adenoma, colorectal, breast and non-small cell lung cancer.
Physical form
Formulated in 25 mM Tris-HCl, pH 8.0, 138 mM NaCl, 0.05% Tween-20, 50% glycerol and 3 mM DTT.
Preparation Note
Thaw on ice. Upon first thaw, briefly spin tube containing enzyme to recover full content of the tube. Aliquot enzyme into single use aliquots. Store remaining undiluted enzyme in aliquots at -70°C. Note: Enzyme is very sensitive to freeze/thaw cycles.
Other Notes
One unit is defined as the amount of enzyme that will phosphorylate 1 pmol of Tyr substrate per minute at pH 7.4 and 30°C.
