EGFR is the receptor for members of the EGF family and is a transmembrane glycoprotein that has tyrosine kinase activity. Binding of epidermal growth factor to EGFR induces receptor dimerization and tyrosine autophosphorylation and leads to cell proliferation, differentiation, motility, and cell survival (1). Activation of EGFR triggers mitogenic signaling in gastrointestinal mucosa, and its expression is upregulated in colon cancers and most neoplasms (2). Activation of EGFR triggers activation of the ERK-signaling pathway in normal gastric epithelial and colon cancer cell lines. Inactivation of EGFR with selective inhibitors significantly reduces ERK2 activation, c-fos mRNA expression and cell proliferation.
ERBB, mENA, ERBB1, HER1
1. Wang K, et al: Epidermal growth factor receptor-deficient mice have delayed primary endochondral ossification because of defective osteoclast recruitment. J. Biol. Chem. 279: 53848-53856, 2004.
2. Kobayashi S, et al: EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. New Eng. J. Med. 352: 786-792, 2005.
Sample Kinase Activity Plot. For specific information on a given lot, see related technical data sheet.
Sample Purity Data. For specific information on a given lot, see related technical data sheet.
Storage, Stability, and Shipping:
Store product at –70oC. For optimal storage, aliquot target into smaller quantities after centrifugation and store at recommended temperature. For most favorable performance, avoid repeated handling and multiple freeze/thaw cycles.
DE Heppner et al., The NADPH Oxidases DUOX1 and NOX2 Play Distinct Roles in Redox Regulation of Epidermal Growth Factor Receptor Signaling. Journal of Biological Chemistry October 2016 10.1074/jbc.M116.749028
Krejci Pavel et al., NF449 Is a Novel Inhibitor of Fibroblast Growth Factor Receptor 3 (FGFR3) Signaling Active in Chondrocytes and Multiple Myeloma Cells Journal of Biological Chemistry July 2010 10.1074/jbc.M109.083626
Shun-Na Ge et al., Hydrogen Sulfide Targets EGFR Cys797/Cys798 Residues to Induce Na+/K+-ATPase Endocytosis and Inhibition in Renal Tubular Epithelial Cells and Increase Sodium Excretion in Chronic Salt-Loaded Rats Antioxidants & Redox Signaling November 2014 10.1089/ars.2013.5304
K Danyal et al., Acrolein and thiol-reactive electrophiles suppress allergen-induced innate airway epithelial responses by inhibition of DUOX1 and EGFR. American Journal of Physiology - Lung Cellular and Molecular Physiology November 2016 10.1152/ajplung.00276.2016
Lia Feng et al., Screening of epidermal growth factor receptor inhibitors in natural products by capillary electrophoresis combined with high performance liquid chromatography-tandem mass spectrometry Journal of Chromatography A June 2015 10.1016/j.chroma.2015.04.055
Rao Suman et al., Target Modulation by a Kinase Inhibitor Engineered to Induce a Tandem Blockade of the Epidermal Growth Factor Receptor (EGFR) and c-Src: The Concept of Type III Combi-Targeting PLoS One February 2015 10.1371/journal.pone.0117215
Krejci Pavel et al., Receptor Tyrosine Kinases Activate Canonical WNT/β-Catenin Signaling via MAP Kinase/LRP6 Pathway and Direct β-Catenin Phosphorylation PLoS One April 2012 10.1371/journal.pone.0035826
AKT/PKB Pathway, Angiogenesis, Apoptosis/Autophagy, Cancer, Cardiovascular Disease, Cell Cycle, ERK/MAPK Pathway, Inflammation, Invasion/Metastasis, Metabolic Disorder, PKA/PKC Pathway, Receptor Tyrosine Kinases