Human EGFR: epidermal growth factor receptor, tyrosine kinase domain, recombinant and active enzyme
The epidermal growth factor receptor (EGFR) is part of the erbB family of receptor tyrosine kinases, including also HER2/erbB2, HER3/erbB3 and HER4/erbB4. Activation of ErbB receptors is initiated by ligand binding to their extracellular domain, leading to the formation of both, homo- and heterodimeric ErbB receptor complexes. Upon dimerization the receptor kinase undergo autophosphorylation at specific tyrosine residues within the intracellular domain, acting as binding sites for proteins e.g. Shc, Grb2, Src, PI3K, SHP1 and SHP2. This couples the ErbB receptor to downstream signaling pathways e.g. MAPK and the Akt pathway, resulting in the activation of target genes within the nucleus, which determine biological responses, such as proliferation or differentiation. Deregulated EGFR signaling, caused by overexpression of the receptor or an enhanced ligand production, is frequent in many tumor types. Thus, there is a great interest in generation of specific inhibitors. Gefitinib (Iressa) is an orally available ATP competitive EGFR-inhibitor which had demonstrated significant efficacy in non-small cell lung cancer.
Specific activity : 23.000 pmol/mg min
Method for determination of Km value & specific activity: Filter binding assay MAFC membrane
Protein concentration: 0.16 mg/ml (Bradford method using BSA as standard protein)
Size: 10 µg
Ordering information: shipped on dry ice
Product specific literature references:
Ono M, Kuwano M.(2006) " Molecular mechanisms of epidermal growth factor receptor (EGFR) activation and response to gefitinib and other EGFR-targeting drugs." Clin Cancer Res, 12(24):7242-51.
Takayuki Fukui, MD · Tetsuya Mitsudomi, MD.(2008) " Mutations in the epidermal growth factor receptor gene and effects of EGFR–tyrosine kinase inhibitors on lung cancers". Gen Thorac Cardiovasc Surg. 56:97–103.
Uberall I, Kolár Z, Trojanec R, Berkovcová J, Hajdúch M.(2008) "The status and role of ErbB receptors in human cancer". Exp Mol Pathol. 84(2):79-89
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