TTD Target ID: TTDS00355

Target Information
Name	Epidermal growth factor receptor
Type of target	Successful target
Synonyms	EGFR
	EGFR-TK
	Epidermal growth factor receptor ErbB-1
	Epidermal growth factor receptor-tyrosine kinase
	Receptor protein-tyrosine kinase ErbB-1
Disease	Breast cancer    [1][2][3]
	Cancer, unspecific    [4][5][6]
	Colorectal cancer    [7]
	Glioblastoma multiforme    [8]
	HCV infection    [9]
	Head and neck tumors    [10]
	Lymphangiomatosis    [11]
	Nonsmall cell lung cancer    [12][13]
	Ovarian cancer    [3]
	Pancreatic cancer    [14]
	Solid tumor    [15][16]
	Squamous cell carcinoma    [17]
	Tumors    [18]
Drug(s)	Cetuximab		Approved	Colorectal Cancer	[17][14][19]
	Lapatinib		Approved	Breast cancer	[20][21]
	Panitumumab		Approved	Colorectal Cancer	[22]
	Tyverb/Tykerb		Approved	Refractory breast cancer	[23]
	DWP-401		Launched	Diabetic foot ulcers	[24]
	Erlotinib		Launched	Non-small cell lung cancer	[25]
	Gefitinib		Launched	Cancers	[26][13]
	HEGF		Launched	Diabetic foot ulcers	[24]
	BIBW 2992		Phase III	Non-small cell lung cancer	[27]
	Erlotinib		Phase III	Pancreatic cancer	[25][28]
	Erlotinib+Bevacizumab		Phase III	NSCLC	[28][29]
	Gefitinib		Phase III	Head & neck cancer	[30][31]
	HKI-272		Phase III	Breast Cancer	[30]
	Pazopanib + Tyverb/Tykerb		Phase III	Inflammatory breast cancer	[23]
	Tykerb		Phase III	Refractory metastatic breast cancer, RCC	[30]
	Tyverb/Tykerb		Phase III	Gastric cancer	[23]
	Vandetanib		Phase III	Solid tumours, NSCLC	[30][31]
	Tykerb		Phase II completed	Bladder, head & neck, NSCLC, brain cancer	[30]
	XL647		Phase II completed	Carcinoma, Non-Small-Cell Lung	[32]
	Bevacizumab+Erlotinib		Phase II	NSCLC	[28]
	Erlotinib		Phase II	Colon, glioma, breast, RCC ovarian, head & neck cancer	[25][28]
	Gefitinib		Phase II	Urethral, bladder, ovarian, prostate, breast cancer	[30][31]
	HKI-272		Phase II	Advanced Malignant Solid Tumors; Breast Cancer	[30]
	PF-299804		Phase II	Cancer	[33][34]
	Panitumumab		Phase II	Locally advanced head and neck cancer	[22][35][36]
	Tyverb/Tykerb		Phase II	Head & neck squamous cell carcinoma	[23]
	Vandetanib		Phase II	Breast, thyroid tumours, multiple myeloma, brain, head & neck cancer	[30][31]
	XL647		Phase I completed	Cancer	[32]
	S-222611		Phase Ib	Malignant tumor	[37]
	Anti-HER3/EGFR DAF		Phase I	Metastatic epithelial tumors	[38]
	AZD4769		Discontinued in Phase I	Solid tumours	[31]
	BMS-599626		Suspended in Phase I	Various cancers	[30]
	CI-1033		Discontinued in Phase II	Cancer, NSCLC; cancer, colorectal; cancer, head and neck; cancer, thyroid; cancer, breast; cancer, mesothelioma; cancer, sarcoma, general; cancer, melanoma	[30]
	TAK165		Suspended in Phase I	Various cancers	[30]
BioChemical Class	Transferases transferring phosphorus-containing groups
EC Number	EC 2.7.1.112
Pathway	Adherens 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 ID	P00533
PDB Structure	1DNQ; 1DNR; 1IVO; 1M14; 1M17; 1MOX; 1NQL; 1XKK.
Function	Receptor 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.
Sequence	MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEV VLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALA VLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDF QNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGC TGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYV VTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFK NCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAF ENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKL FGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCN LLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVM GENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVV ALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGS GAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGI CLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAA RNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSY GVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPK FRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQ QGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTED SIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLN TVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRV APQSSEFIGA
Related US Patent	6,551,989
	6,566,324
	6,638,543
Target Validation	Click to Find Target Validation Information.
QSAR Model	Click to Find Target QSAR Model.
Inhibitor	AG-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]
Antibody	ABX-EGF		[18]
	Anti-HER3/EGFR DAF		[38]
	Cetuximab		[17][14][19]
	EMD 55900		[18]
	ICR 62		[18]
Activator	DWP-401		[24]
	HEGF		[24]
Suppressor	Panitumumab		[22]
	Panitumumab		[22][35][36]
Multitarget	Anti-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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Professor in Department of Pharmacy
National University of Singapore, Singapore

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