Therapeutic Targets Database
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TTD Target ID: TTDS00249

Target Information
NameReceptor protein-tyrosine kinase erbB-2    
Type of targetSuccessful target    
SynonymsC-erbB-2    
C-erbB-2 oncoprotein    
ERBB2    
Epidermal growth factor receptor 2    
Erb2    
HER-2    
HER2 (erbB2/neu)    
HER2/neu    
MLN 19    
NEU proto-oncogene    
P185erbB2    
Tyrosine kinase receptor ErbB2    
Tyrosine kinase-type cell surface receptor HER2    
DiseaseBreast cancer
[ICD9: 174, 175   ICD10: C50]
[1][2][3]
Cancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[4][5][6]
Colon cancer
[ICD9: 153, 154   ICD10: C18-C21]
[7]
Ependymoma
[ICD9: 191, 225   ICD10: C71, D33]
[8]
Ovarian cancer
[ICD9: 183   ICD10: C56]
[9]
Drug(s)LapatinibApprovedBreast cancer[10][11]
TrastuzumabApprovedBreast cancer[12][13][1]
Tyverb/TykerbApprovedRefractory breast cancer[14]
BIBW 2992Phase IIINon-small cell lung cancer[15]
Bevacizumab+TrastuzumabPhase IIIMetastatic breast cancer[16]
HKI-272Phase IIIBreast Cancer[17]
Pazopanib + Tyverb/TykerbPhase IIIInflammatory breast cancer[14]
PertuzumabPhase IIIBreast Cancer[16][18]
RG1273Phase IIIEarly HER2-positive breast cancer
Trastuzumab-DM1Phase IIIBreast Cancer[19][20]
TykerbPhase IIIRefractory metastatic breast cancer, RCC[17]
Tyverb/TykerbPhase IIIGastric cancer[14]
TykerbPhase II completedBladder, head & neck, NSCLC, brain cancer[17]
XL647Phase II completedCarcinoma, Non-Small-Cell Lung[21]
AZD8931Phase IINeoplasms; Breast Neoplasms; Breast Cancer[22][23]
HKI-272Phase IIAdvanced Malignant Solid Tumors; Breast Cancer[17]
PertuzumabPhase IIPancreatic Cancer[16][18]
Tyverb/TykerbPhase IIHead & neck squamous cell carcinoma[14]
XL647Phase I completedCancer[21]
S-222611Phase IbMalignant tumor[24]
ARRY-380Phase IBreast cancer
MGAH22Phase ISolid Tumors
MM-302Phase IBreast cancer
TAK-285Phase ISolid tumors[25]
BMS-599626Suspended in Phase IVarious cancers[17]
CI-1033Discontinued in Phase IICancer, NSCLC; cancer, colorectal; cancer, head and neck; cancer, thyroid; cancer, breast; cancer, mesothelioma; cancer, sarcoma, general; cancer, melanoma[17]
CP-724714DiscontinuedVarious cancers[17]
TAK165Suspended in Phase IVarious cancers[17]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.112
PathwayAdherens junction
Bladder cancer
Calcium signaling pathway
Endometrial cancer
ErbB signaling pathway
Focal adhesion
Non-small cell lung cancer
Pancreatic cancer
Pathways in cancer
Prostate cancer
UniProt IDP04626
PDB Structure1MFG; 1MFL; 1MW4; 1N8Z; 1OVC; 1QR1; 1S78; 2A91; 2JWA; 2KS1; 2L4K; 3BE1; 3H3B; 3MZW; 3N85; 3PP0; 3RCD.    
FunctionEssential component of a neuregulin-receptor complex, althought neuregulins do not interact with it alone. Gp30 is a potential ligand for this receptor. not activated by EGF, EGF-alpha and amphiregulin.    
SequenceMELAALCRWGLLLALLPPGAASTQVCTGTDMKLRLPASPETHLDMLRHLYQGCQVVQGNL ELTYLPTNASLSFLQDIQEVQGYVLIAHNQVRQVPLQRLRIVRGTQLFEDNYALAVLDNG DPLNNTTPVTGASPGGLRELQLRSLTEILKGGVLIQRNPQLCYQDTILWKDIFHKNNQLA LTLIDTNRSRACHPCSPMCKGSRCWGESSEDCQSLTRTVCAGGCARCKGPLPTDCCHEQC AAGCTGPKHSDCLACLHFNHSGICELHCPALVTYNTDTFESMPNPEGRYTFGASCVTACP YNYLSTDVGSCTLVCPLHNQEVTAEDGTQRCEKCSKPCARVCYGLGMEHLREVRAVTSAN IQEFAGCKKIFGSLAFLPESFDGDPASNTAPLQPEQLQVFETLEEITGYLYISAWPDSLP DLSVFQNLQVIRGRILHNGAYSLTLQGLGISWLGLRSLRELGSGLALIHHNTHLCFVHTV PWDQLFRNPHQALLHTANRPEDECVGEGLACHQLCARGHCWGPGPTQCVNCSQFLRGQEC VEECRVLQGLPREYVNARHCLPCHPECQPQNGSVTCFGPEADQCVACAHYKDPPFCVARC PSGVKPDLSYMPIWKFPDEEGACQPCPINCTHSCVDLDDKGCPAEQRASPLTSIISAVVG ILLVVVLGVVFGILIKRRQQKIRKYTMRRLLQETELVEPLTPSGAMPNQAQMRILKETEL RKVKVLGSGAFGTVYKGIWIPDGENVKIPVAIKVLRENTSPKANKEILDEAYVMAGVGSP YVSRLLGICLTSTVQLVTQLMPYGCLLDHVRENRGRLGSQDLLNWCMQIAKGMSYLEDVR LVHRDLAARNVLVKSPNHVKITDFGLARLLDIDETEYHADGGKVPIKWMALESILRRRFT HQSDVWSYGVTVWELMTFGAKPYDGIPAREIPDLLEKGERLPQPPICTIDVYMIMVKCWM IDSECRPRFRELVSEFSRMARDPQRFVVIQNEDLGPASPLDSTFYRSLLEDDDMGDLVDA EEYLVPQQGFFCPDPAPGAGGMVHHRHRSSSTRSGGGDLTLGLEPSEEEAPRSPLAPSEG AGSDVFDGDLGMGAAKGLQSLPTHDPSPLQRYSEDPTVPLPSETDGYVAPLTCSPQPEYV NQPDVRPQPPSPREGPLPAARPAGATLERPKTLSPGKNGVVKDVFAFGGAVENPEYLTPQ GGAAPQPHPPPAFSPAFDNLYYWDQDPPERGAPPSTFKGTPTAENPEYLGLDVPV
Target ValidationClick to Find Target Validation Information.    
Inhibitor (1-Benzyl-1H-indazol-5-yl)-quinazolin-4-yl-amine[26]
(1-Benzyl-1H-indol-5-yl)-quinazolin-4-yl-amine[26]
AZD8931[22][23]
BIBW 2992[15]
BMS-599626[17]
CI-1033[17]
CP-724714[17]
HKI-272[17]
Lapatinib[10][11]
Pazopanib + Tyverb/Tykerb[14]
Pertuzumab[16][18]
S-222611[24]
TAK-285[25]
TAK165[17]
Tykerb[17]
Tyverb/Tykerb[14]
WAY-177820[8]
XL647[21]
AntibodyAnti-ErbB-2 monoclonal antibody[1]
Bevacizumab+Trastuzumab[16]
Herceptin[1]
Mini-antibody (scFv)[4]
Trastuzumab[12][13][1]
Trastuzumab-DM1[19][20]
InducerRhuMAb HER2[2]
MultitargetBIBW 2992[15]
BMS-599626[17]
Bevacizumab+Trastuzumab[16]
CI-1033[17]
HKI-272[17]
Lapatinib[10][11]
Pazopanib + Tyverb/Tykerb[14]
S-222611[24]
TAK165[17]
Tykerb[17]
Tyverb/Tykerb[14]
XL647[21]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Anti-ErbB-2 monoclonal antibodies and ErbB-2-directed vaccines. Cancer Immunol Immunother. 2002 Jan;50(11):569-87. Epub 2001 Nov 24. To Reference
Ref 2The basic biology of HER2. Ann Oncol. 2001;12 Suppl 1:S3-8. To Reference
Ref 3Comparative multi-methodological measurement of ERBB2 status in breast cancer. J Pathol. 2004 Mar;202(3):286-98. To Reference
Ref 4A new human antitumor immunoreagent specific for ErbB2. Clin Cancer Res. 2002 Jun;8(6):1710-9. To Reference
Ref 5Growth factor receptors as therapeutic targets: strategies to inhibit the insulin-like growth factor I receptor. Oncogene. 2003 Sep 29;22(42):6589-97. To Reference
Ref 6Generation of monoclonal antibody CIBCgp185 against C-erbB-2 oncoprotein and its clinical evaluation. Hum Antibodies. 2001;10(3-4):101-7. To Reference
Ref 7Effects of trastuzumab on epidermal growth factor receptor-dependent and -independent human colon cancer cells. Int J Cancer. 2004 Mar 20;109(2):291-301. To Reference
Ref 8ERBB receptor signaling promotes ependymoma cell proliferation and represents a potential novel therapeutic target for this disease. Clin Cancer Res. 2002 Oct;8(10):3054-64. To Reference
Ref 9HER-2 overexpression is an independent marker of poor prognosis of advanced primary ovarian carcinoma: a multicenter study of the GINECO group. Ann Oncol. 2004 Jan;15(1):104-12. To Reference
Ref 10Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7. To Reference
Ref 11Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42. Epub 2006 Nov 28. To Reference
Ref 12Her2/neu is not a commonly expressed therapeutic target in melanoma -- a large cohort tissue microarray study. Melanoma Res. 2004 Jun;14(3):207-10. To Reference
Ref 13Nat Rev Drug Discov. 2003 Jan;2(1):38-51.Knockouts model the 100 best-selling drugs--will they model the next 100? To Reference
Ref 14GSK. Product Development Pipeline. February 2009. To Reference
Ref 15Boehringer Ingelheim. Product Development Pipeline. June 2 2009. To Reference
Ref 16Roche. Product Development Pipeline. July 29 2009. To Reference
Ref 17A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. To Reference
Ref 18Roche. Report of Roche. 2008. To Reference
Ref 19Genentech. Product Development Pipeline. July 2009. To Reference
Ref 20Trastuzumab--mechanism of action and use in clinical practice. N Engl J Med. 2007 Jul 5;357(1):39-51. To Reference
Ref 21Combined inhibition of vascular endothelial growth factor and epidermal growth factor signaling in non-small-cell lung cancer therapy. Clin Lung Cancer. 2009 Mar;10 Suppl 1:S17-23. To Reference
Ref 22AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 23Characterization of AZD8931, a potent reversible small molecule inhibitor against epidermal growth factor receptor (EGFR), erythroblastic leukemia viral oncogene homolog 2 (HER2) and 3 (HER3) with a unique and balanced pharmacological profile. J Clin Oncol 27:15s, 2009 To Reference
Ref 242011 Pipeline of Shionogi. To Reference
Ref 25Takeda. Product Development Pipeline. July 31 2009. To Reference
Ref 26Bioorg Med Chem Lett. 2001 Jun 4;11(11):1401-5.Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2. To Reference



 

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