Target Information

Target General Infomation
Target ID
T14597
Former ID
TTDS00249
Target Name
Receptor protein-tyrosine kinase erbB-2
Gene Name
ERBB2
Synonyms
C-erbB-2; C-erbB-2 oncoprotein; 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; ERBB2
Target Type
Successful
Disease Advanced breast cancer [ICD9: 174, 175; ICD10: C50]
Asthma; Breast cancer [ICD9:174, 175; ICD10: J45, C50]
Breast cancer; Gastric cancer [ICD9:174, 175, 151; ICD10: C50, C16]
Breast cancer [ICD9: 174, 175; ICD10: C50]
Bladder cancer [ICD9: 188; ICD10: C67]
Colorectal cancer; HER2-positive urogenital cancer [ICD9:153, 154, 179-186; ICD10: C18-C21, C50-C68]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Glioblastoma multiforme [ICD9: 191; ICD10: C71]
Gastric cancer [ICD9: 151; ICD10: C16]
Gastrointestinal cancers [ICD9: 150-159; ICD10: C15-C26]
Head and neck squamous cell carcinoma [ICD9: 199; ICD10: C44]
Inflammatory breast cancer [ICD9: 174, 175; ICD10: C50]
Lymphoma [ICD9: 202.8, 208.9; ICD10: C81-C86]
Malignant tumor [ICD9: 140-199; ICD10: C00-C75, C7A, C7B]
Metastatic breast cancer [ICD10: C50]
Non-hodgkin's lymphoma [ICD10: C85]
Non-small cell lung cancer [ICD10: C33-C34]
Prostate cancer [ICD9: 185; ICD10: C61]
Retinal venous occlusion [ICD10: H34.8]
Refractory breast cancer [ICD9: 174, 175; ICD10: C50]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Unspecified [ICD code not available]
Function
In the nucleus is involved intranscriptional regulation. Associates with the 5'-TCAAATTC-3' sequence in the PTGS2/COX-2 promoter and activates its transcription. Implicated in transcriptional activation of CDKN1A; the function involves STAT3 and SRC. Involved in the transcription of rRNA genes by RNA Pol I and enhances protein synthesis and cell growth.
BioChemical Class
Kinase
Target Validation
T14597
UniProt ID
P04626
EC Number
EC 2.7.10.1
Sequence
MELAALCRWGLLLALLPPGAASTQVCTGTDMKLRLPASPETHLDMLRHLYQGCQVVQGNL
ELTYLPTNASLSFLQDIQEVQGYVLIAHNQVRQVPLQRLRIVRGTQLFEDNYALAVLDNG
DPLNNTTPVTGASPGGLRELQLRSLTEILKGGVLIQRNPQLCYQDTILWKDIFHKNNQLA
LTLIDTNRSRACHPCSPMCKGSRCWGESSEDCQSLTRTVCAGGCARCKGPLPTDCCHEQC
AAGCTGPKHSDCLACLHFNHSGICELHCPALVTYNTDTFESMPNPEGRYTFGASCVTACP
YNYLSTDVGSCTLVCPLHNQEVTAEDGTQRCEKCSKPCARVCYGLGMEHLREVRAVTSAN
IQEFAGCKKIFGSLAFLPESFDGDPASNTAPLQPEQLQVFETLEEITGYLYISAWPDSLP
DLSVFQNLQVIRGRILHNGAYSLTLQGLGISWLGLRSLRELGSGLALIHHNTHLCFVHTV
PWDQLFRNPHQALLHTANRPEDECVGEGLACHQLCARGHCWGPGPTQCVNCSQFLRGQEC
VEECRVLQGLPREYVNARHCLPCHPECQPQNGSVTCFGPEADQCVACAHYKDPPFCVARC
PSGVKPDLSYMPIWKFPDEEGACQPCPINCTHSCVDLDDKGCPAEQRASPLTSIISAVVG
ILLVVVLGVVFGILIKRRQQKIRKYTMRRLLQETELVEPLTPSGAMPNQAQMRILKETEL
RKVKVLGSGAFGTVYKGIWIPDGENVKIPVAIKVLRENTSPKANKEILDEAYVMAGVGSP
YVSRLLGICLTSTVQLVTQLMPYGCLLDHVRENRGRLGSQDLLNWCMQIAKGMSYLEDVR
LVHRDLAARNVLVKSPNHVKITDFGLARLLDIDETEYHADGGKVPIKWMALESILRRRFT
HQSDVWSYGVTVWELMTFGAKPYDGIPAREIPDLLEKGERLPQPPICTIDVYMIMVKCWM
IDSECRPRFRELVSEFSRMARDPQRFVVIQNEDLGPASPLDSTFYRSLLEDDDMGDLVDA
EEYLVPQQGFFCPDPAPGAGGMVHHRHRSSSTRSGGGDLTLGLEPSEEEAPRSPLAPSEG
AGSDVFDGDLGMGAAKGLQSLPTHDPSPLQRYSEDPTVPLPSETDGYVAPLTCSPQPEYV
NQPDVRPQPPSPREGPLPAARPAGATLERPKTLSPGKNGVVKDVFAFGGAVENPEYLTPQ
GGAAPQPHPPPAFSPAFDNLYYWDQDPPERGAPPSTFKGTPTAENPEYLGLDVPV
Structure
1MFG; 1MFL; 1MW4; 1N8Z; 1OVC; 1QR1; 1S78; 2A91; 2JWA; 2KS1; 2L4K; 3BE1; 3H3B; 3MZW; 3N85; 3PP0; 3RCD; 4GFU; 4HRL; 4HRM; 4HRN; 1MFG; 1MFL; 1MW4; 1N8Z; 1OVC;1QR1; 1S78; 2A91; 2JWA; 2KS1; 2L4K; 3BE1; 3H3B; 3MZW; 3N85; 3PP0; 3RCD; 4GFU; 4HRL; 4HRM; 4HRN
Drugs and Mode of Action
Drug(s) BIBW 2992 Drug Info Approved Non-small cell lung cancer [1], [2]
Lapatinib Drug Info Approved Breast cancer [3], [4]
Masoprocol Drug Info Approved Prostate cancer [5], [6]
Pertuzumab Drug Info Approved Breast cancer [7], [8]
Trastuzumab Drug Info Approved Asthma; Breast cancer [9], [10], [6]
Tyverb/Tykerb Drug Info Approved Refractory breast cancer [11]
Bevacizumab + Trastuzumab Drug Info Phase 3 Metastatic breast cancer [12]
Dacomitinib Drug Info Phase 3 Non-small cell lung cancer [13], [14]
HKI-272 Drug Info Phase 3 Breast cancer [15]
Nelipepimut Drug Info Phase 3 Non-hodgkin's lymphoma [16]
NeuVax Drug Info Phase 3 Breast cancer [16]
PF-05280014 Drug Info Phase 3 Breast cancer [17]
Taxol/Paraplatin/Herceptin Drug Info Phase 3 Breast cancer [18]
Trastuzumab-DM1 Drug Info Phase 3 Breast cancer [19]
Tyverb/Tykerb Drug Info Phase 3 Gastric cancer [11]
Anti-CD3 and anti-Her2/neu bispecific antibody-armed activated T cells Drug Info Phase 2 Breast cancer [20]
AZD8931 Drug Info Phase 2 Breast cancer [21], [22]
Bevacizumab + Trastuzumab Drug Info Phase 2 Breast cancer [23]
BMS-599626 Drug Info Phase 2 Solid tumours [24], [25]
CI-1033 Drug Info Phase 2 Lymphoma [26], [27]
CP-724714 Drug Info Phase 2 Lymphoma [28], [29]
DN24-02 Drug Info Phase 2 Colorectal cancer; HER2-positive urogenital cancer [30]
Ertumaxomab Drug Info Phase 2 Breast cancer [31], [32]
HER-2 Protein AutoVac Drug Info Phase 2 Breast cancer [33]
Her2-targeted autologous T-cell therapy Drug Info Phase 2 Glioblastoma multiforme [34]
HER2/neu peptide vaccine Drug Info Phase 2 Breast cancer [35]
HM-78136B Drug Info Phase 2 Solid tumours [36], [37]
Margetuximab Drug Info Phase 2 Gastrointestinal cancers [38], [39]
MGAH22 Drug Info Phase 2 Solid tumours [38]
MM-111 Drug Info Phase 2 Breast cancer; Gastric cancer [40]
Pazopanib + Tyverb/Tykerb Drug Info Phase 2 Inflammatory breast cancer [41]
Tyverb/Tykerb Drug Info Phase 2 Head and neck squamous cell carcinoma [11]
ABY-025 Drug Info Phase 1/2 Bladder cancer [42]
AGN-208397 Drug Info Phase 1/2 Retinal venous occlusion [43]
AVX901 Drug Info Phase 1/2 Breast cancer [44]
Varlitinib Drug Info Phase 1/2 Breast cancer [45], [46]
S-222611 Drug Info Phase 1b Malignant tumor [47]
ARRY-380 Drug Info Phase 1 Cancer [48]
Cipatinib Drug Info Phase 1 Cancer [49]
CUDC-101 Drug Info Phase 1 Solid tumours [50]
Ertumaxomab Drug Info Phase 1 Advanced breast cancer [51]
HER2p63-71 peptide vaccine Drug Info Phase 1 Cancer [52]
JNJ-26483327 Drug Info Phase 1 Cancer [53]
MM-302 Drug Info Phase 1 Breast cancer [54]
MVA HER-2 AutoVac Drug Info Phase 1 Breast cancer [55]
Recombinant human Erbb3 fragment therapeutic tumor vaccine Drug Info Phase 1 Cancer [56]
TAK-285 Drug Info Phase 1 Cancer [57]
TrasGEX Drug Info Phase 1 Cancer [58]
VM-206 Drug Info Phase 1 Cancer [59]
Zemab Drug Info Phase 1 Cancer [60]
Her-2-Bi-armed ATC Drug Info Discontinued in Phase 2 Breast cancer [61]
TAK165 Drug Info Discontinued in Phase 1 Cancer [62], [63]
GW-974 Drug Info Terminated Breast cancer [64]
Inhibitor (1-Benzyl-1H-indazol-5-yl)-quinazolin-4-yl-amine Drug Info [65]
(1-Benzyl-1H-indol-5-yl)-quinazolin-4-yl-amine Drug Info [65]
AGN-208397 Drug Info [66]
AVX901 Drug Info [44]
AZD8931 Drug Info [67], [68]
BIBW 2992 Drug Info [69]
BMS-599626 Drug Info [70]
CI-1033 Drug Info [70]
CP-724714 Drug Info [70]
GW-974 Drug Info [71]
HER-2 Protein AutoVac Drug Info [33]
Her2-targeted autologous T-cell therapy Drug Info [72]
HKI-272 Drug Info [70]
HM-78136B Drug Info [73]
JNJ-26483327 Drug Info [74]
Lapatinib Drug Info [75], [76]
Nelipepimut Drug Info [77]
Pazopanib + Tyverb/Tykerb Drug Info [78]
Pertuzumab Drug Info [79], [80]
S-222611 Drug Info [47]
TAK-285 Drug Info [81]
TAK165 Drug Info [70]
Taxol/Paraplatin/Herceptin Drug Info [82]
Tyverb/Tykerb Drug Info [78]
Enhancer ABY-025 Drug Info [83]
Modulator ARRY-380 Drug Info [84]
Cipatinib Drug Info [85]
CUDC-101 Drug Info [50]
DN24-02 Drug Info [86]
Masoprocol Drug Info [87]
MGAH22 Drug Info [88]
MM-111 Drug Info [89]
MM-302 Drug Info [90]
PF 5208766 Drug Info
Varlitinib Drug Info [85]
Antagonist Dacomitinib Drug Info [14]
PF-05280014 Drug Info [91]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
DRM DRM Info
Pathways
KEGG Pathway ErbB signaling pathway
Calcium signaling pathway
HIF-1 signaling pathway
Focal adhesion
Adherens junction
Pathways in cancer
Proteoglycans in cancer
MicroRNAs in cancer
Pancreatic cancer
Endometrial cancer
Prostate cancer
Bladder cancer
Non-small cell lung cancer
Central carbon metabolism in cancer
NetPath Pathway TCR Signaling Pathway
PANTHER Pathway Cadherin signaling pathway
EGF receptor signaling pathway
Pathway Interaction Database ErbB4 signaling events
ErbB2/ErbB3 signaling events
ErbB receptor signaling network
a6b1 and a6b4 Integrin signaling
Validated targets of C-MYC transcriptional repression
PathWhiz Pathway Phosphatidylinositol Phosphate Metabolism
Reactome SHC1 events in ERBB2 signaling
PLCG1 events in ERBB2 signaling
PIP3 activates AKT signaling
GRB2 events in ERBB2 signaling
PI3K events in ERBB2 signaling
Constitutive Signaling by Aberrant PI3K in Cancer
Sema4D induced cell migration and growth-cone collapse
RAF/MAP kinase cascade
WikiPathways DNA Damage Response (only ATM dependent)
ErbB Signaling Pathway
EGF/EGFR Signaling Pathway
Focal Adhesion
Extracellular vesicle-mediated signaling in recipient cells
Bladder Cancer
Signaling by ERBB2
Integrated Pancreatic Cancer Pathway
Signaling Pathways in Glioblastoma
Leptin signaling pathway
miR-targeted genes in muscle cell - TarBase
Semaphorin interactions
References
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REF 2(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5667).
REF 3FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022059.
REF 4(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5692).
REF 5(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4265).
REF 6Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
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REF 8Pertuzumab, trastuzumab, and docetaxel for HER2-positive metastatic breast cancer (CLEOPATRA study): overall survival results from a randomised, double-blind, placebo-controlled, phase 3 study. Lancet Oncol. 2013 May;14(6):461-71.
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REF 11FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022059.
REF 12AVEREL: a randomized phase III Trial evaluating bevacizumab in combination with docetaxel and trastuzumab as first-line therapy for HER2-positive locally recurrent/metastatic breast cancer. J Clin Oncol. 2013 May 10;31(14):1719-25.
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REF 28ClinicalTrials.gov (NCT00102895) A Research Study of CP-724,714 in Patients With HER2 Overexpressing Metastatic Breast Cancer. U.S. National Institutes of Health.
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REF 38ClinicalTrials.gov (NCT01828021) Phase 2 Study of the Monoclonal Antibody MGAH22 (Margetuximab) in Patients With Relapsed or Refractory Advanced Breast Cancer. U.S. National Institutes of Health.
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REF 40ClinicalTrials.gov (NCT01774851) A Study of MM-111 and Paclitaxel With Trastuzumab in Patients HER2 Positive Carcinomas of the Distal Esophagus, Gastroesophageal (GE) Junction and Stomach. U.S. National Institutes of Health.
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