Pages
Products

EGFR


Official Full Name
epidermal growth factor receptor
Organism
Homo sapiens
Gene ID
1956
Background
The protein encoded by this gene is a transmembrane glycoprotein that is a member of the protein kinase superfamily. This protein is a receptor for members of the epidermal growth factor family. EGFR is a cell surface protein that binds to epidermal growth factor, thus inducing receptor dimerization and tyrosine autophosphorylation leading to cell proliferation. Mutations in this gene are associated with lung cancer. EGFR is a component of the cytokine storm which contributes to a severe form of Coronavirus Disease 2019 (COVID-19) resulting from infection with severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). [provided by RefSeq, Jul 2020]
Synonyms
ERBB; ERRP; HER1; mENA; ERBB1; NNCIS; PIG61; NISBD2
Bio Chemical Class
Kinase
Protein Sequence
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFKNCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAFENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKLFGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCNLLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVMGENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVVALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
Open
Disease
Lung cancer, Melanoma
Approved Drug
20 +
Clinical Trial Drug
85 +
Discontinued Drug
9 +

Cat.No. Product Name Price
CSC-DC004772 Panoply™ Human EGFR Knockdown Stable Cell Line Inquiry
CSC-RO0741 Human EGFR-L858R-L718Q Stable Cell Line - Ba/F3 Inquiry
CSC-RO0740 Human EGFR-L858R-T790M-L718V Stable Cell Line - Ba/F3 Inquiry
CSC-RO0739 Human EGFR-Del19-T790M-L718V Stable Cell Line - Ba/F3 Inquiry
CSC-RO0738 Human EGFR-L718V Stable Cell Line - Ba/F3 Inquiry
CSC-RO0737 Human EGFR-Del19-T790M-L718Q Stable Cell Line - Ba/F3 Inquiry
CSC-RO0722 Human EGFR-A763-Y764insFQEA-C797S Stable Cell Line - Ba/F3 Inquiry
CSC-RO0718 Human EGFR-D770-N771insSVD-C797S Stable Cell Line - Ba/F3 Inquiry
CSC-RO0717 Human EGFR-V769-D770insASV-C797S Stable Cell Line - Ba/F3 Inquiry
CSC-RO0716 Human EGFR-Del19-C797S Stable Cell Line - PC-9 Inquiry
CSC-RO0714 Human EGFR-L718Q Stable Cell Line - Ba/F3 Inquiry
CSC-RO0456 Human EGFR-Del19/T790M/C797S Stable Cell Line - PC-9 Inquiry
CSC-RO0455 Human EGFR-T790M/C797S/L858R Stable Cell Line - NCI-H1975 Inquiry
CSC-RO0451 Human EGFR Stable Cell Line - CT26 Inquiry
CSC-RO0450 Human EGFR Stable Cell Line - MC38 Inquiry
CSC-RO0449 Human EGFR-V3 Stable Cell Line - A375 Inquiry
CSC-RO0438 Human EGFR vIII Stable Cell Line - HEK293T Inquiry
CSC-RO0433 Human EGFR-V3 Stable Cell Line - CHO-K1 Inquiry
CSC-RO0324 Human EGFR-P772-H773_ins_NPH Stable Cell Line - Ba/F3 Inquiry
CSC-RO0323 Human EGFR_G724S Stable Cell Line - Ba/F3 Inquiry
CSC-RO0322 Human EGFR-Y764-V765_ins_HH Stable Cell Line - Ba/F3 Inquiry
CSC-RO0321 Human EGFR-H773-V774_ins_PH Stable Cell Line - Ba/F3 Inquiry
CSC-RO0320 Human EGFR-D770-N771_ins_NPG Stable Cell Line - Ba/F3 Inquiry
CSC-RO0319 Human EGFR-A767-S768_ins_TLA Stable Cell Line - Ba/F3 Inquiry
CSC-RO0742 Human EGFR-Del19-L718V Stable Cell Line - Ba/F3 Inquiry
CSC-RO0318 Human EGFR-D770-N771_ins_GF Stable Cell Line - Ba/F3 Inquiry
CSC-RO0743 Human EGFR-L858R-L718V Stable Cell Line - Ba/F3 Inquiry
CSC-RO0772 Human EGFR-L858R/T790M/L792H Stable Cell Line - Ba/F3 Inquiry
CSC-RT2769 Human EGFR Knockout Cell Line-HEK293T Inquiry
CSC-RO1065 Human EGFR Stable Cell Line-CHO-K1(GS-/-) Inquiry
CSC-RO0834 Human EGFR-Del19-G724S-T790M Stable Cell Line - Ba/F3 Inquiry
CSC-RO0827 Human EGFR-A763-Y764insFQEA-T790M Stable Cell Line - Ba/F3 Inquiry
CSC-RO0826 Human EGFR-D770-N771insSVD-T790M Stable Cell Line - Ba/F3 Inquiry
CSC-RO0825 Human EGFR-V769-D770insASV-T790M Stable Cell Line - Ba/F3 Inquiry
CSC-RO0824 Human EGFR-H773-V774insNPH-T790M Stable Cell Line - Ba/F3 Inquiry
CSC-RO0801 Human EGFR-E709H Stable Cell Line - Ba/F3 Inquiry
CSC-RO0800 Human EGFR-E709K/T790M/L858R Stable Cell Line - Ba/F3 Inquiry
CSC-RO0799 Human EGFR-T790M/L858R/L718Q Stable Cell Line - Ba/F3 Inquiry
CSC-RO0798 Human EGFR-L747S/G719A Stable Cell Line - Ba/F3 Inquiry
CSC-RO0797 Human EGFR-L747S Stable Cell Line - Ba/F3 Inquiry
CSC-RO0796 Human EGFR-E709K/L858R Stable Cell Line - Ba/F3 Inquiry
CSC-RO0795 Human EGFR-L747S/L858R Stable Cell Line - Ba/F3 Inquiry
CSC-RO0794 Human EGFR-E709K/G719A Stable Cell Line - Ba/F3 Inquiry
CSC-RO0793 Human EGFR-E709V Stable Cell Line - Ba/F3 Inquiry
CSC-RO0792 Human EGFR-L747V Stable Cell Line - Ba/F3 Inquiry
CSC-RO0791 Human EGFR-E709-710>D Stable Cell Line - Ba/F3 Inquiry
CSC-RO0790 Human EGFR-E709-710>G Stable Cell Line - Ba/F3 Inquiry
CSC-RO0789 Human EGFR-E709-710>M Stable Cell Line - Ba/F3 Inquiry
CSC-RO0786 Human EGFR-E709Q Stable Cell Line - Ba/F3 Inquiry
CSC-RO0785 Human EGFR-E709A Stable Cell Line - Ba/F3 Inquiry
CSC-RO0784 Human EGFR-E709G Stable Cell Line - Ba/F3 Inquiry
CSC-RO0767 Human EGFR-L858R/T790M/G796R Stable Cell Line - Ba/F3 Inquiry
CSC-RT2770 Human EGFR Knockout Cell Line-PC3 Inquiry
CSC-RO0317 Human EGFR-K745-E746_ins_IPVAIK Stable Cell Line - Ba/F3 Inquiry
CSC-RO0315 Human EGFR-K745-E746_ins_VPVAIK Stable Cell Line - Ba/F3 Inquiry
CLOE-1813 Human EGFR Insect Cell Lysate Inquiry
CSC-RT2588 Human EGFR Knockout Cell Line-A549 Inquiry
CSC-RT1811 EGFR Knockout Cell Line-HeLa Inquiry
CSC-RO0239 Human EGFR-Del19/T790M/L858R Stable Cell Line-Ba/F3 Inquiry
CSC-SC004772 Panoply™ Human EGFR Over-expressing Stable Cell Line Inquiry
CSC-RO0143 Human EGFR-T790M/L861Q Stable Cell Line-Ba/F3 Inquiry
CSC-RO0142 Human EGFR-T790M/C797S Stable Cell Line-Ba/F3 Inquiry
CSC-RO0141 Human EGFR-T790M Stable Cell Line-Ba/F3 Inquiry
CSC-RO0140 Human EGFR-L861Q Stable Cell Line-Ba/F3 Inquiry
CSC-RO0139 Human EGFR-L858R/T790M/C797S Stable Cell Line-Ba/F3 Inquiry
CSC-RO0138 Human EGFR-L858R/T790M Stable Cell Line-Ba/F3 Inquiry
CSC-RO0137 Human EGFR-L858R/C797S Stable Cell Line-Ba/F3 Inquiry
CSC-RO0136 Human EGFR-L858R Stable Cell Line-Ba/F3 Inquiry
CSC-RO0135 Human EGFR-H773_V774insNPH Stable Cell Line-Ba/F3 Inquiry
CSC-RO0134 Human EGFR-G719S/T263P Stable Cell Line-Ba/F3 Inquiry
CSC-RO0133 Human EGFR-G719S Stable Cell Line-Ba/F3 Inquiry
CSC-RO0132 Human EGFR-DEL19/T790M/C797S Stable Cell Line-Ba/F3 Inquiry
CSC-RO0131 Human EGFR-DEL19/T790M Stable Cell Line-Ba/F3 Inquiry
CSC-RO0130 Human EGFR-DEL19/C797S Stable Cell Line-Ba/F3 Inquiry
CSC-RO0129 Human EGFR-DEL19 Stable Cell Line-Ba/F3 Inquiry
CSC-RO0128 Human EGFR-D770_N771insSVD Stable Cell Line-Ba/F3 Inquiry
CSC-RO0127 Human EGFR-C797S Stable Cell Line-Ba/F3 Inquiry
CSC-RO0126 Human EGFR Stable Cell Line-Ba/F3 Inquiry
CLOE-1814 Human EGFR HEK293 Cell Lysate Inquiry
CSC-RO0316 Human EGFR-V769-D770_ins_GE Stable Cell Line - Ba/F3 Inquiry
CLOE-1815 Human EGFR(His) Insect Cell Lysate Inquiry
CLOE-2140 Rat Egfr (His) HEK293 Cell Lysate Inquiry
CSC-RO0314 Human EGFR-P772-H773_ins_NP Stable Cell Line - Ba/F3 Inquiry
CSC-RO0313 Human EGFR-I744-K745_ins_KIPVAI Stable Cell Line - Ba/F3 Inquiry
CSC-RO0312 Human EGFR-N771-P772_ins_N Stable Cell Line - Ba/F3 Inquiry
CSC-RO0311 Human EGFR-D770-N771_ins_GT Stable Cell Line - Ba/F3 Inquiry
CSC-RO0310 Human EGFR-D770-N771_ins_Y Stable Cell Line - Ba/F3 Inquiry
CSC-RO0309 Human EGFR-H773-V774_ins_AH Stable Cell Line - Ba/F3 Inquiry
CSC-RO0308 Human EGFR-V774-C775_ins_HV Stable Cell Line - Ba/F3 Inquiry
CSC-RO0307 Human EGFR-H773-V774_ins_H Stable Cell Line - Ba/F3 Inquiry
CSC-RO0306 Human EGFR-D770del_ins_GY Stable Cell Line - Ba/F3 Inquiry
CSC-RO0305 Human EGFR-N771del_ins_GY Stable Cell Line - Ba/F3 Inquiry
CSC-RO0304 Human EGFR-N771-P772_ins_H Stable Cell Line - Ba/F3 Inquiry
CSC-RO0303 Human EGFR-D770_N771insG Stable Cell Line - Ba/F3 Inquiry
CSC-RO0302 Human EGFR-A763_Y764insFQEA Stable Cell Line - Ba/F3 Inquiry
CSC-RO0301 Human EGFR-A289V Stable Cell Line - Ba/F3 Inquiry
CSC-RO0300 Human EGFR-A289D Stable Cell Line - Ba/F3 Inquiry
CSC-RO0299 Human EGFR-A289T Stable Cell Line - Ba/F3 Inquiry
CSC-RO0298 Human EGFR_S768I Stable Cell Line - Ba/F3 Inquiry
CSC-RO0297 Human EGFR-V769_D770insASV Stable Cell Line - Ba/F3 Inquiry
CSC-RO0296 Human EGFR-P699_N700insASV Stable Cell Line - Ba/F3 Inquiry
CSC-RO0295 Human EGFR-VIII Stable Cell Line - Ba/F3 Inquiry
CLKO-1660 EGFR KO Cell Lysate-HeLa Inquiry
CLOE-2308 Mouse Egfr(Fc) HEK293 Cell Lysate Inquiry
CLOE-2307 Mouse Egfr HEK293 Cell Lysate Inquiry
CLOE-1816 Human EGFR(Fc) HEK293 Cell Lysate Inquiry
CSC-RT2795 Human EGFR Knockout Cell Line-T47D Inquiry

Detailed Information

The epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase within the ErbB family consisting of 4 members; EGFR (ErbB1, HER1), ErbB2 (HER2), ErbB3 (HER3), and ErbB4 (HER4). In many different cancer cell types, the ErbB pathway becomes hyperactivated by a series of mechanisms, including overproduction of ligands, overproduction of receptors, or constitutive activation of receptors. Generally, EGFR signaling is triggered by ligand binding to the extracellular ligand binding domain. The typically known ligands are EGF, TGF-alpha, betacellulin, amphiregulin and epiregulin. This initiates receptor homo-/hetero-dimerization and autophosphorylation through the intracellular kinase domain, leading to receptor activation. Following activation, cytoplasmic substrates are phosphorylated and initiate a signaling cascade that drives various cellular responses, including changes in gene expression, apoptosis inhibition, cytoskeletal rearrangement, and increased cell proliferation.

EGFRFigure 1. EGFR and its signal pathway. (Huang L, Fu L. 2015)

The role of EGFR in cancer

Due to its important role in cell survival, proliferation, angiogenesis, and cell differentiation, EGFR-amplification and mutations are key triggers in multiple human cancer cells. Upregulation of the EGFR signaling pathway might result in increased cell growth and proliferation as well as a high potential for the rapid formation of metastases. Overexpression of EGFR, found in bladder, esophageal, cervical, ovarian and head and neck tumors, typically correlates with poor prognosis reflected in the unfavorable progression free survival (PFS) and overall survival (OS) in 70 % of studies. In addition, activating somatic EGFR mutations, especially found in non-small cell lung cancer (NSCLC) patients, nowadays suggest a higher response rate (RR) to tyrosine kinase inhibitors (TKIs) therapies than standard chemotherapy and generally lead to a better prognosis with prolonged PFS compared to patients bearing wild type (WT) EGFR. These activating mutations can act as a predictive factor for prognosis under TKI therapy. This development of dependencies of cancer cells on specific oncogenic signals (like EGFR) may be powerful targets for pharmacotherapy. Finally, this anti-EGF therapy results in tumor cell death induced by BIM, a family member of BCL-2.

EGFR inhibitors and cancer treatment

Targeting the EGFR pathway is a strategy for cancer therapy, including monoclonal antibodies directed against the extracellular domain of the receptor and small molecules inhibiting specific EGFR tyrosine kinases (EGFR-TKIs). Erlotinib and gefitinib are both inhibitors of the tyrosine kinase activity of EGFR and compete with ATP in binding to the tyrosine kinase pocket of the receptor. They have been extensively studied in patients with NSCLC. The presence of somatic mutations in the kinase domain of EGFR, including deletions in exon 19 of the EGFR gene and replacement of leucine with arginine at codon 858, is closely associated with a positive response to gefitinib and erlotinib in NSCLC patients. Despite the benefits of EGFR-TKI in the treatment of NSCLC, most patients finally develop resistance to these drugs. Besides, in other cancers, the efficacy of EGFR-TKIs is low.

Cetuximab, a monoclonal antibody that binds to EGFR, has a higher affinity than the original ligands, prevents receptor activation, inhibits cell proliferation and angiogenesis and promotes antibody-dependent cellular cytotoxicity. Currently, cetuximab is used in combination with either chemotherapy or radiotherapy to treat colorectal and head and neck cancers. However, patients with KRAS mutation may exhibit resistance to cetuximab treatment. Hence, identification of novel strategies or agents to overcome innate and acquired resistance to EGFR-TKIs and cetuximab is an important clinical goal.

Novel strategies that, potentially combined with earlier EGFR-targeting agents, result in enhanced cell killing are therefore still desired. Current research has shown that EGFR-deregulated cells and tumors display alterations in their autophagic response, a pro-survival mechanism that allows cells to recycle nutrients for energy- and macromolecule production. Importantly: (1) EGFR-deregulated cells seem to be more dependent on autophagy for survival and growth; and (2) resistance to EGFR-targeting agents can be reduced by autophagy inhibition, providing a potential novel modality to target these tumors.

References:

  1. Jutten B, Rouschop K. EGFR signaling and autophagy dependence for growth, survival, and therapy resistance. Cell cycle, 2014, 13(1): 42-51.
  2. Juchum M, et al. Fighting cancer drug resistance: Opportunities and challenges for mutation-specific EGFR inhibitors. Drug Resistance Updates, 2015, 20: 12-28.
  3. Cui J, et al. EGFR inhibitors and autophagy in cancer treatment. Tumor Biology, 2014, 35(12): 11701-11709.
  4. Huang L, Fu L. Mechanisms of resistance to EGFR tyrosine kinase inhibitors. Acta Pharmaceutica Sinica B, 2015, 5(5): 390-401.
Quick Inquiry