Therapeutic Targets Database
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TTD Target ID: TTDS00355

Target Information
NameEpidermal growth factor receptor    
Type of targetSuccessful target    
SynonymsEGFR    
EGFR-TK    
Epidermal growth factor receptor ErbB-1    
Epidermal growth factor receptor-tyrosine kinase    
Receptor protein-tyrosine kinase ErbB-1    
DiseaseBreast cancer
[ICD9: 174, 175   ICD10: C50]
[1][2][3]
Cancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[4][5][6]
Colorectal cancer
[ICD9: 153, 154   ICD10: C18-C21]
[7]
Glioblastoma multiforme
[ICD9: 191   ICD10: C71]
[8]
HCV infection
[ICD9: 070.4, 070.5, 070.70   ICD10: B17.1, B18.2]
[9]
Head and neck tumors
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[10]
Lymphangiomatosis[11]
Nonsmall cell lung cancer
[ICD9: 140-229, 162, 204.0   ICD10: C00-C96, C33-C34, C91.0]
[12][13]
Ovarian cancer
[ICD9: 183   ICD10: C56]
[3]
Pancreatic cancer
[ICD9: 157   ICD10: C25]
[14]
Solid tumor
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[15][16]
Squamous cell carcinoma
[ICD9: 199   ICD10: C44]
[17]
Tumors
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[18]
Drug(s)CetuximabApprovedColorectal Cancer[17][14][19]
LapatinibApprovedBreast cancer[20][21]
PanitumumabApprovedColorectal Cancer[22]
Tyverb/TykerbApprovedRefractory breast cancer[23]
DWP-401LaunchedDiabetic foot ulcers[24]
ErlotinibLaunchedNon-small cell lung cancer[25]
GefitinibLaunchedCancers[26][13]
HEGFLaunchedDiabetic foot ulcers[24]
BIBW 2992Phase IIINon-small cell lung cancer[27]
DE-766Phase IIIGastric cancer
DE-766Phase IIINon small cell lung cancer
ErlotinibPhase IIIPancreatic cancer[25][28]
Erlotinib+BevacizumabPhase IIINSCLC[28][29]
GefitinibPhase IIIHead & neck cancer[30][31]
HKI-272Phase IIIBreast Cancer[30]
NecitumumabPhase IIISquamous non-small cell lung cancer
Pazopanib + Tyverb/TykerbPhase IIIInflammatory breast cancer[23]
RindopepimutPhase IIIFront-line glioblastoma
TykerbPhase IIIRefractory metastatic breast cancer, RCC[30]
Tyverb/TykerbPhase IIIGastric cancer[23]
VandetanibPhase IIISolid tumours, NSCLC[30][31]
TykerbPhase II completedBladder, head & neck, NSCLC, brain cancer[30]
XL647Phase II completedCarcinoma, Non-Small-Cell Lung[32]
Bevacizumab+ErlotinibPhase IINSCLC[28]
ErlotinibPhase IIColon, glioma, breast, RCC ovarian, head & neck cancer[25][28]
GefitinibPhase IIUrethral, bladder, ovarian, prostate, breast cancer[30][31]
HKI-272Phase IIAdvanced Malignant Solid Tumors; Breast Cancer[30]
MEHD7945APhase IIColorectal cancer
MEHD7945APhase IIHead and neck cancer
PF-299804Phase IICancer[33][34]
PanitumumabPhase IILocally advanced head and neck cancer[22][35][36]
RG7160Phase IISecond-line metastatic colorectal
RG7160Phase IISolid tumors
RG7597Phase IIHead and neck cancer
RG7597Phase IIMetastatic epithelial tumors
RindopepimutPhase IIRecurrent glioblastoma
Tyverb/TykerbPhase IIHead & neck squamous cell carcinoma[23]
VandetanibPhase IIBreast, thyroid tumours, multiple myeloma, brain, head & neck cancer[30][31]
CO-1686Phase I/IISecond-line NSCLC
XL647Phase I completedCancer[32]
S-222611Phase IbMalignant tumor[37]
ABT-806Phase ISolid Tumors
AMG 595Phase IGlioblastoma
Anti-HER3/EGFR DAFPhase IMetastatic epithelial tumors[38]
DE-766Phase IEsophageal cancer
MEHD7945APhase IMetastatic epithelial tumors
MM-151Phase ISolid Tumors
AZD4769Discontinued in Phase ISolid tumours[31]
BMS-599626Suspended in Phase IVarious cancers[30]
CI-1033Discontinued in Phase IICancer, NSCLC; cancer, colorectal; cancer, head and neck; cancer, thyroid; cancer, breast; cancer, mesothelioma; cancer, sarcoma, general; cancer, melanoma[30]
TAK165Suspended in Phase IVarious cancers[30]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.112
PathwayAdherens junction
Bladder cancer
Calcium signaling pathway
Colorectal cancer
Cytokine-cytokine receptor interaction
Endometrial cancer
Epithelial cell signaling in Helicobacter pylori
ErbB signaling pathway
Focal adhesion
Gap junction
Glioma
GnRH signaling pathway
MAPK signaling pathway
Melanoma
Non-small cell lung cancer
Pancreatic cancer
Pathways in cancer
Prostate cancer
Regulation of actin cytoskeleton
UniProt IDP00533
PDB Structure1DNQ; 1DNR; 1IVO; 1M14; 1M17; 1MOX; 1NQL; 1XKK; 1YY9; 1Z9I; 2EB2; 2EB3; 2EXP; 2EXQ; 2GS2; 2GS6; 2GS7; 2ITN; 2ITO; 2ITP; 2ITQ; 2ITT; 2ITU; 2ITV; 2ITW; 2ITX; 2ITY; 2ITZ; 2J5E; 2J5F; 2J6M; 2JIT; 2JIU; 2JIV; 2KS1; 2M20; 2RF9; 2RFD; 2RFE; 2RGP; 3B2U; 3B2V; 3BEL; 3BUO; 3C09; 3G5V; 3G5Y; 3GOP; 3GT8; 3IKA; 3LZB; 3NJP; 3OB2; 3OP0; 3P0Y; 3PFV; 3POZ; 3QWQ; 3UG1; 3UG2; 3VJN; 3VJO; 3VRP; 3VRR; 3W2O; 3W2P; 3W2Q; 3W2R; 3W2S; 3W32; 3W33; 4G5J; 4G5P; 4HJO; 4I1Z; 4I20; 4I21; 4I22; 4I23; 4I24.    
FunctionReceptor for egf, but also for other members of the egf family, as tgf-alpha, amphiregulin, betacellulin, heparin-binding egf-like growth factor, gp30 and vaccinia virus growth factor. Is involved in the control of cell growth and differentiation.    
SequenceMRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEV VLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALA VLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDF QNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGC TGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYV VTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFK NCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAF ENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKL FGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCN LLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVM GENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVV ALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGS GAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGI CLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAA RNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSY GVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPK FRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQ QGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTED SIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLN TVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRV APQSSEFIGA
Related US Patent6,551,989
6,566,324
6,638,543
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
InhibitorAG-213[39]
AG-490[40]
AG-538[40]
AZD-0530[41]
AZD4769[31]
BIBW 2992[27]
BMS-599626[30]
Bevacizumab+Erlotinib[28]
CGP-53353[42]
CI-1033[30]
CL-387785[43]
CP-358774[44]
Erlotinib[25][28]
Erlotinib[25]
Erlotinib+Bevacizumab[28][29]
Flavopiridol[45]
Gefitinib[26][13]
Gefitinib[30][31]
HKI-272[30]
HTS-00213[43]
HTS-02876[43]
HTS-05058[46]
IMC-C225[14]
LAVENDUSTIN A[47]
Lapatinib[20][21]
Lapatinib ditosylate[48]
NERATINIB[49]
OSI-75[4]
PD-0166326,   PD-166326[50]
PD-0173956[50]
PD-0180970[50]
PD-153035[51]
PD-158780[52]
PD-168393[53]
PD182905[54]
PF-299804[33][34]
PKI-166[54]
Pazopanib + Tyverb/Tykerb[23]
RG-50810[40]
Ro-4396686[55]
S-222611[37]
SKI-758[56]
TAK165[30]
TYRPHOSTIN AG-1478[57]
Tykerb[30]
Tyverb/Tykerb[23]
VATALANIB[49]
Vandetanib[30][31]
XL647[32]
cochliobolic acid[58]
AntibodyABX-EGF[18]
Anti-HER3/EGFR DAF[38]
Cetuximab[17][14][19]
EMD 55900[18]
ICR 62[18]
ActivatorDWP-401[24]
HEGF[24]
SuppressorPanitumumab[22][35][36]
Panitumumab[22]
MultitargetAnti-HER3/EGFR DAF[38]
BIBW 2992[27]
BMS-599626[30]
Bevacizumab+Erlotinib[28]
CI-1033[30]
Erlotinib+Bevacizumab[28][29]
HKI-272[30]
Lapatinib[20][21]
Pazopanib + Tyverb/Tykerb[23]
S-222611[37]
TAK165[30]
Tykerb[30]
Tyverb/Tykerb[23]
Vandetanib[30][31]
XL647[32]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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Ref 2Epidermal growth factor receptor expression is a candidate target of the synergistic combination of trastuzumab and flavopiridol in breast cancer. Cancer Res. 2003 Jul 1;63(13):3626-31. To Reference
Ref 3Allelic length of a CA dinucleotide repeat in the egfr gene correlates with the frequency of amplifications of this sequence--first results of an inter-ethnic breast cancer study. J Pathol. 2004 May;203(1):545-50. To Reference
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Ref 7Epidermal growth factor receptor expression and measurement in solid tumors. Semin Oncol. 2002 Oct;29(5 Suppl 14):45-54. To Reference
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Ref 29Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science. 2004 Aug 20;305(5687):1163-7. Epub 2004 Jul 29. To Reference
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Ref 41J Med Chem. 2006 Nov 2;49(22):6465-88.N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. To Reference
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Professor in Department of Pharmacy
National University of Singapore, Singapore


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