Merck, E2645-500UN, Epidermal Growth Factor Receptor human

General description
Research area: Cell signaling

Epidermal growth factor receptor (EGFR) belongs to a family of cell surface receptors called receptor tyrosine kinases (RTKs) and is also the most studied member of this family. The EGFR is encoded by the ErbB gene, mapped to chromosome 7 q22. These receptors are attached to the cytoplasmic membrane and consist of an ectodomain (ECD), comprising of four subdomains called DI-DIV, a hydrophobic transmembrane domain, and an intracytoplasmic tyrosine kinase domain.
Biochem/physiol Actions
170 kDa glycoprotein having EGF-activated protein tyrosine kinase activity; high levels of EGFR are expressed in approximately one third of human epithelial tumors, and in the cancers of the bladder, breast or lung that have poor clinical prognosis.
EGF exerts its actions by binding to the EGF receptor (EGFR), a 170 kDa glycoprotein having EGF-activated protein tyrosine kinase activity. Even in the absence of EGF-like ligands, EGFR can participate in cellular responses elicited by several other stimuli. High levels of EGFR are expressed in approximately one third of human epithelial tumors, and in the cancers of the bladder, breast or lung that have poor clinical prognosis, hence the interest in targeting EGFR.
Epidermal growth factor receptor (EGFR) has an essential role in normal developmental processes, and is mutated in multiple cancers. It is involved in the pathogenesis of epidermoid tumors, and thus, has extreme importance as a cancer therapeutic target. Gefitinib (GEF) and erlotinib act as EGFR inhibitors, and induce apoptosis in non-small cell lung cancer (NSCLC) cells. A truncated isoform, called EGFRvIII is linked to multiple cases of head and neck squamous cell carcinoma (HNSCC). In ∼40% of glioblastoma multiforme (GBM), this gene is amplified.
Physical form
Lyophilized from a solution in 50 mM HEPES, pH 7.6, 150 mM NaCl, 0.05% Triton X-100, 1 mM dithiothreitol, and 10% trehalose.
Preparation Note
Affinity purified from human carcinoma A431 cells.
Other Notes
One unit (U) of the enzyme is defined as the amount needed to incorporate 1 pmol of phosphate into the substrate (KVEKIGEGTYGVVYK: 6 - 20 residue of p34cdc2) in 1 minute.