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]
Bladder cancer [ICD9: 188; ICD10: C67]
Breast cancer; Gastric cancer [ICD9:174, 175, 151; ICD10: C50, C16]
Breast cancer [ICD9: 174, 175; ICD10: C50]
Colorectal cancer; HER2-positive urogenital cancer [ICD9:153, 154, 179-186; ICD10: C18-C21, C50-C68]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Gastrointestinal cancers [ICD9: 150-159; ICD10: C15-C26]
Glioblastoma multiforme [ICD9: 191; ICD10: C71]
Gastric cancer [ICD9: 151; ICD10: C16]
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 [529823], [541010]
Lapatinib Drug Info Approved Breast cancer [538586], [541034]
Masoprocol Drug Info Approved Prostate cancer [467601], [536361]
Pertuzumab Drug Info Approved Breast cancer [468138], [532320]
Trastuzumab Drug Info Approved Asthma; Breast cancer [468150], [532651], [536361]
Tyverb/Tykerb Drug Info Approved Refractory breast cancer [538585]
Bevacizumab + Trastuzumab Drug Info Phase 3 Metastatic breast cancer [532301]
Dacomitinib Drug Info Phase 3 Non-small cell lung cancer [523496], [542446]
HKI-272 Drug Info Phase 3 Breast cancer [548009]
Nelipepimut Drug Info Phase 3 Non-hodgkin's lymphoma [523700]
NeuVax Drug Info Phase 3 Breast cancer [523700]
PF-05280014 Drug Info Phase 3 Breast cancer [524830]
Taxol/Paraplatin/Herceptin Drug Info Phase 3 Breast cancer [528260]
Trastuzumab-DM1 Drug Info Phase 3 Breast cancer [532548]
Tyverb/Tykerb Drug Info Phase 3 Gastric cancer [538585]
Anti-CD3 and anti-Her2/neu bispecific antibody-armed activated T cells Drug Info Phase 2 Breast cancer [549995]
AZD8931 Drug Info Phase 2 Breast cancer [524722], [542691]
Bevacizumab + Trastuzumab Drug Info Phase 2 Breast cancer [554002]
BMS-599626 Drug Info Phase 2 Solid tumours [523940], [542630]
CI-1033 Drug Info Phase 2 Lymphoma [525738], [541018]
CP-724714 Drug Info Phase 2 Lymphoma [521628], [542808]
DN24-02 Drug Info Phase 2 Colorectal cancer; HER2-positive urogenital cancer [523475]
Ertumaxomab Drug Info Phase 2 Breast cancer [529707], [531972]
HER-2 Protein AutoVac Drug Info Phase 2 Breast cancer [531718]
Her2-targeted autologous T-cell therapy Drug Info Phase 2 Glioblastoma multiforme [532563]
HER2/neu peptide vaccine Drug Info Phase 2 Breast cancer [524128]
HM-78136B Drug Info Phase 2 Solid tumours [524875], [542826]
Margetuximab Drug Info Phase 2 Gastrointestinal cancers [524257], [543243]
MGAH22 Drug Info Phase 2 Solid tumours [524257]
MM-111 Drug Info Phase 2 Breast cancer; Gastric cancer [524196]
Pazopanib + Tyverb/Tykerb Drug Info Phase 2 Inflammatory breast cancer [532156]
Tyverb/Tykerb Drug Info Phase 2 Head and neck squamous cell carcinoma [538585]
ABY-025 Drug Info Phase 1/2 Bladder cancer [524300]
AGN-208397 Drug Info Phase 1/2 Retinal venous occlusion [522883]
AVX901 Drug Info Phase 1/2 Breast cancer [523789]
Varlitinib Drug Info Phase 1/2 Breast cancer [522608], [542628]
S-222611 Drug Info Phase 1b Malignant tumor [551683]
ARRY-380 Drug Info Phase 1 Cancer [524395]
Cipatinib Drug Info Phase 1 Cancer [523370]
CUDC-101 Drug Info Phase 1 Solid tumours [533101]
Ertumaxomab Drug Info Phase 1 Advanced breast cancer [889343]
HER2p63-71 peptide vaccine Drug Info Phase 1 Cancer [525850]
JNJ-26483327 Drug Info Phase 1 Cancer [522319]
MM-302 Drug Info Phase 1 Breast cancer [523378]
MVA HER-2 AutoVac Drug Info Phase 1 Breast cancer [523092]
Recombinant human Erbb3 fragment therapeutic tumor vaccine Drug Info Phase 1 Cancer [551788]
TAK-285 Drug Info Phase 1 Cancer [522127]
TrasGEX Drug Info Phase 1 Cancer [523579]
VM-206 Drug Info Phase 1 Cancer [524352]
Zemab Drug Info Phase 1 Cancer [548526]
Her-2-Bi-armed ATC Drug Info Discontinued in Phase 2 Breast cancer [548761]
TAK165 Drug Info Discontinued in Phase 1 Cancer [541276], [547786]
GW-974 Drug Info Terminated Breast cancer [546750]
Inhibitor (1-Benzyl-1H-indazol-5-yl)-quinazolin-4-yl-amine Drug Info [526072]
(1-Benzyl-1H-indol-5-yl)-quinazolin-4-yl-amine Drug Info [526072]
AGN-208397 Drug Info [532414]
AVX901 Drug Info [523789]
AZD8931 Drug Info [550278], [550288]
BIBW 2992 Drug Info [550386]
BMS-599626 Drug Info [536474]
CI-1033 Drug Info [536474]
CP-724714 Drug Info [536474]
GW-974 Drug Info [550119]
HER-2 Protein AutoVac Drug Info [531718]
Her2-targeted autologous T-cell therapy Drug Info [532879]
HKI-272 Drug Info [536474]
HM-78136B Drug Info [531542]
JNJ-26483327 Drug Info [550422]
Lapatinib Drug Info [536331], [537224]
Nelipepimut Drug Info [532798]
Pazopanib + Tyverb/Tykerb Drug Info [550963]
Pertuzumab Drug Info [549951], [551607]
S-222611 Drug Info [551683]
TAK-285 Drug Info [551717]
TAK165 Drug Info [536474]
Taxol/Paraplatin/Herceptin Drug Info [527947]
Tyverb/Tykerb Drug Info [550963]
Enhancer ABY-025 Drug Info [530980]
Modulator ARRY-380 Drug Info [549731]
Cipatinib Drug Info [1572591]
CUDC-101 Drug Info [533101]
DN24-02 Drug Info [528989]
Masoprocol Drug Info [556264]
MGAH22 Drug Info [544225]
MM-111 Drug Info [889442]
MM-302 Drug Info [533224]
PF 5208766 Drug Info
Varlitinib Drug Info [1572591]
Antagonist Dacomitinib Drug Info [542446]
PF-05280014 Drug Info [532875]
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
Ref 467601(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 468138(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: 5046).
Ref 468150(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: 5082).
Ref 521628ClinicalTrials.gov (NCT00102895) A Research Study of CP-724,714 in Patients With HER2 Overexpressing Metastatic Breast Cancer. U.S. National Institutes of Health.
Ref 522127ClinicalTrials.gov (NCT00535522) A Safety and Pharmacokinetic Study of TAK-285 in Patients With Advanced Cancer. U.S. National Institutes of Health.
Ref 522319ClinicalTrials.gov (NCT00676299) A Safety and Dose-finding Study of JNJ-26483327, a Drug in Development for Cancer, for Patients With Advanced and/or Refractory Solid Malignancies.. U.S. National Institutes of Health.
Ref 522608ClinicalTrials.gov (NCT00862524) A Study of ARRY-334543 and Gemcitabine in Patients With Advanced Cancer and Pancreatic Cancer. U.S. National Institutes of Health.
Ref 522883ClinicalTrials.gov (NCT01027650) Safety and Efficacy of AGN208397 in the Treatment of Macular Edema Associated With Retinal Vein Occlusion (RVO). U.S. National Institutes of Health.
Ref 523092ClinicalTrials.gov (NCT01152398) A Safety and Immunology Study of a Modified Vaccinia Vaccine for HER-2(+) Breast Cancer After Adjuvant Therapy. U.S. National Institutes of Health.
Ref 523370ClinicalTrials.gov (NCT01301911) Study of Cipatinib in Patients With HER2 Positive or Uncertain Advanced Breast Cancer. U.S. National Institutes of Health.
Ref 523378ClinicalTrials.gov (NCT01304797) Safety and Pharmacokinetic Study of MM-302 in Patients With Advanced Breast Cancer. U.S. National Institutes of Health.
Ref 523475ClinicalTrials.gov (NCT01353222) DN24-02 as Adjuvant Therapy in Subjects With High Risk HER2+ Urothelial Carcinoma. U.S. National Institutes of Health.
Ref 523496ClinicalTrials.gov (NCT01360554) ARCHER 1009 : A Study Of Dacomitinib (PF-00299804) Vs. Erlotinib In The Treatment Of Advanced Non-Small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 523579ClinicalTrials.gov (NCT01409343) TrasGEX Dose Escalation Study. U.S. National Institutes of Health.
Ref 523700ClinicalTrials.gov (NCT01479244) Efficacy and Safety Study of NeuVax (Nelipepimut-S or E75) Vaccine to Prevent Breast Cancer Recurrence. U.S. National Institutes of Health.
Ref 523789ClinicalTrials.gov (NCT01526473) A Phase I Study To Evaluate The Antitumor Activity And Safety Of AVX901. U.S. National Institutes of Health.
Ref 523940ClinicalTrials.gov (NCT01614522) A Clinical Trial Evaluating the Effect of ASLAN001 in Patients With Recurrent/Metastatic Gastric Cancer Whose Tumors Are Either HER-2 Amplified or Co-expressing HER-1and HER-2. U.S. National Institutes of Health.
Ref 524128ClinicalTrials.gov (NCT01729884) Vaccine Therapy in Treating Patients With Stage IV Hormone Receptor Positive Breast Cancer. U.S. National Institutes of Health.
Ref 524196ClinicalTrials.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.
Ref 524257ClinicalTrials.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.
Ref 524300ClinicalTrials.gov (NCT01858116) PET Study of Breast Cancer Patients Using [68Ga]ABY-025. U.S. National Institutes of Health.
Ref 524352ClinicalTrials.gov (NCT01895491) Safety Study of VM206RY in Subjects With Expression of HER2 in Breast Cancer. U.S. National Institutes of Health.
Ref 524395ClinicalTrials.gov (NCT01921335) ARRY-380 + Trastuzuamab for Breast w/ Brain Mets. U.S. National Institutes of Health.
Ref 524722ClinicalTrials.gov (NCT02117167) Intergroup Trial UNICANCER UC 0105-1305/ IFCT 1301: Efficacy of Targeted Drugs Guided by Genomic Profils in Metastatic NSCLC Patients. U.S. National Institutes of Health.
Ref 524830ClinicalTrials.gov (NCT02187744) A Study Of PF-05280014 Or Trastuzumab Plus Taxotere And Carboplatin In HER2 Positive Breast Cancer In The Neoadjuvant Setting (REFLECTIONS B327-04). U.S. National Institutes of Health.
Ref 524875ClinicalTrials.gov (NCT02216916) Phase II Trial of HM781-36B in Patients With Metastatic/Recurrent Head and Neck Squamous Cell Carcinoma (HNSCC) After Failure of or Unfit for Platinum-containing Therapy. U.S. National Institutes of Health.
Ref 525738Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions. J Med Chem. 2000 Apr 6;43(7):1380-97.
Ref 525850Development of a cancer vaccine: peptides, proteins, and DNA. Cancer Chemother Pharmacol. 2000;46 Suppl:S77-82.
Ref 528260Randomized phase III study of trastuzumab, paclitaxel, and carboplatin compared with trastuzumab and paclitaxel in women with HER-2-overexpressing metastatic breast cancer. J Clin Oncol. 2006 Jun 20;24(18):2786-92.
Ref 529707Ertumaxomab: a trifunctional antibody for breast cancer treatment. Expert Opin Investig Drugs. 2008 Oct;17(10):1553-8.
Ref 529823BIBW-2992, a dual receptor tyrosine kinase inhibitor for the treatment of solid tumors. Curr Opin Investig Drugs. 2008 Dec;9(12):1336-46.
Ref 531718Treatment of HER2-positive breast cancer: current status and future perspectives. Nat Rev Clin Oncol. 2011 Nov 29;9(1):16-32.
Ref 531972Trifunctional antibody ertumaxomab: Non-immunological effects on Her2 receptor activity and downstream signaling. MAbs. 2012 Sep-Oct;4(5):614-22.
Ref 532156A randomized phase II study of lapatinib + pazopanib versus lapatinib in patients with HER2+ inflammatory breast cancer. Breast Cancer Res Treat. 2013 Jan;137(2):471-82.
Ref 532301AVEREL: 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.
Ref 532320Pertuzumab, 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.
Ref 532548Patient-reported outcomes from EMILIA, a randomized phase 3 study of trastuzumab emtansine (T-DM1) versus capecitabine and lapatinib in human epidermal growth factor receptor 2-positive locally advanced or metastatic breast cancer. Cancer. 2014 Mar 1;120(5):642-51.
Ref 532563Adoptive cell therapies for glioblastoma. Front Oncol. 2013 Nov 11;3:275.
Ref 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 533101A Phase I Study of CUDC-101, a Multitarget Inhibitor of HDACs, EGFR, and HER2, in Combination with Chemoradiation in Patients with Head and Neck Squamous Cell Carcinoma. Clin Cancer Res. 2015 Apr 1;21(7):1566-73.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 538585FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022059.
Ref 538586FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022059.
Ref 541010(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 541018(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: 5675).
Ref 541034(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 541276(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: 6011).
Ref 542446(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: 7422).
Ref 542628(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: 7645).
Ref 542630(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: 7647).
Ref 542691(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: 7717).
Ref 542808(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: 7883).
Ref 542826(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: 7903).
Ref 543243(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: 8686).
Ref 546750Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010108)
Ref 547786Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019257)
Ref 548009Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021154)
Ref 548526Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026315)
Ref 548761Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028450)
Ref 549995Journal of Clinical Oncology, 2008 ASCO Annual Meeting Proceedings (Post-Meeting Edition), Vol 26, No 15S (May 20 Supplement), 2008: 3034.
Ref 551683Clinical pipeline report, company report or official report of Shionogi (2011).
Ref 551788Clinical pipeline report, company report or official report of Zensun.
Ref 554002ClinicalTrials.gov (NCT00365365) Safety & Efficacy of Three Docetaxel-Based Chemotherapy Regimens Plus Bevacizumab With or Without Trastuzumab for Adjuvant Treatment of Patients With Breast Cancer
Ref 889343ClinicalTrials.gov (NCT00452140) Phase II Study With the Trifunctional Antibody Ertumaxomab to Treat Metastatic Breast Cancer Progressing After Endocrine Treatment
Ref
Ref 523789ClinicalTrials.gov (NCT01526473) A Phase I Study To Evaluate The Antitumor Activity And Safety Of AVX901. U.S. National Institutes of Health.
Ref 525850Development of a cancer vaccine: peptides, proteins, and DNA. Cancer Chemother Pharmacol. 2000;46 Suppl:S77-82.
Ref 526063Use of anti-CD3 x anti-HER2/neu bispecific antibody for redirecting cytotoxicity of activated T cells toward HER2/neu+ tumors. J Hematother Stem Cell Res. 2001 Apr;10(2):247-60.
Ref 526072Bioorg Med Chem Lett. 2001 Jun 4;11(11):1401-5.Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.
Ref 527947Two concurrent phase II trials of paclitaxel/carboplatin/trastuzumab (weekly or every-3-week schedule) as first-line therapy in women with HER2-overexpressing metastatic breast cancer: NCCTG study 983252. Clin Breast Cancer. 2005 Dec;6(5):425-32.
Ref 528989Treatment with autologous antigen-presenting cells activated with the HER-2 based antigen Lapuleucel-T: results of a phase I study in immunologic and clinical activity in HER-2 overexpressing breast cancer. J Clin Oncol. 2007 Aug 20;25(24):3680-7.
Ref 529707Ertumaxomab: a trifunctional antibody for breast cancer treatment. Expert Opin Investig Drugs. 2008 Oct;17(10):1553-8.
Ref 530257N-terminally LRMK-linked HER-2 peptides, AE-37 [p776(774-788)] and AE-47 [Ava-F7(776-788)], aid differentiation of E75-TCR+CD8+ cells to perforin-positive cells. Anticancer Res. 2009 Jul;29(7):2427-35.
Ref 530980Targeting of HER2-expressing tumors using 111In-ABY-025, a second-generation affibody molecule with a fundamentally reengineered scaffold. J Nucl Med. 2010 Jul;51(7):1131-8.
Ref 531542Antitumor activity of HM781-36B, a highly effective pan-HER inhibitor in erlotinib-resistant NSCLC and other EGFR-dependent cancer models. Int J Cancer. 2012 May 15;130(10):2445-54.
Ref 531718Treatment of HER2-positive breast cancer: current status and future perspectives. Nat Rev Clin Oncol. 2011 Nov 29;9(1):16-32.
Ref 531972Trifunctional antibody ertumaxomab: Non-immunological effects on Her2 receptor activity and downstream signaling. MAbs. 2012 Sep-Oct;4(5):614-22.
Ref 532308Active immunotherapy in HER2 overexpressing breast cancer: current status and future perspectives. Ann Oncol. 2013 Jul;24(7):1740-8.
Ref 532414New hope for dry AMD. Nat Rev Drug Discov. 2013 Jul;12(7):501-2.
Ref 532798The HER2 peptide nelipepimut-S (E75) vaccine (NeuVax?? in breast cancer patients at risk for recurrence: correlation of immunologic data with clinical response. Immunotherapy. 2014;6(5):519-31.
Ref 532875Comparative nonclinical assessments of the proposed biosimilar PF-05280014 and trastuzumab (Herceptin(?)). BioDrugs. 2014 Oct;28(5):451-9.
Ref 532879A new hope in immunotherapy for malignant gliomas: adoptive T cell transfer therapy. J Immunol Res. 2014;2014:326545.
Ref 533101A Phase I Study of CUDC-101, a Multitarget Inhibitor of HDACs, EGFR, and HER2, in Combination with Chemoradiation in Patients with Head and Neck Squamous Cell Carcinoma. Clin Cancer Res. 2015 Apr 1;21(7):1566-73.
Ref 533224Whole-body organ-level and kidney micro-dosimetric evaluations of (64)Cu-loaded HER2/ErbB2-targeted liposomal doxorubicin ((64)Cu-MM-302) in rodents and primates. EJNMMI Res. 2015 Apr 14;5:24.
Ref 535355Anti-ErbB-2 monoclonal antibodies and ErbB-2-directed vaccines. Cancer Immunol Immunother. 2002 Jan;50(11):569-87. Epub 2001 Nov 24.
Ref 535479A new human antitumor immunoreagent specific for ErbB2. Clin Cancer Res. 2002 Jun;8(6):1710-9.
Ref 535660Knockouts model the 100 best-selling drugs--will they model the next 100? Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
Ref 535976Her2/neu is not a commonly expressed therapeutic target in melanoma -- a large cohort tissue microarray study. Melanoma Res. 2004 Jun;14(3):207-10.
Ref 536331Multi-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.
Ref 536448Trastuzumab--mechanism of action and use in clinical practice. N Engl J Med. 2007 Jul 5;357(1):39-51.
Ref 536474A 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.
Ref 537224Triple 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.
Ref 542446(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: 7422).
Ref 544199Immunotoxins and Anticancer Drug Conjugate Assemblies: The Role of the Linkage between Components. Toxins (Basel) 2011 July; 3(7): 848-883.
Ref 544225Anti-tumor activity and toxicokinetics analysis of MGAH22, an anti-HER2 monoclonal antibody with enhanced Fcgamma receptor binding properties. Breast Cancer Res. 2011; 13(6): R123.
Ref 544342Cancer therapy with bispecific antibodies: Clinical experience. Curr Opin Mol Ther. 2010 June; 12(3): 340-349.
Ref 549684J Clin Oncol 31, 2013 (suppl; abstr 3004).
Ref 549692J Clin Oncol 32:5s, 2014 (suppl; abstr 2515).
Ref 549731ARRY-380, a Potent, Small Molecule Inhibitor of ErbB2, Increases Survival in Intracranial ErbB2+ Xenograft Models in Mice
Ref 549951Pertuzumab. Drugs Fut 2008, 33(2): 123 ISSN 0377-8282.
Ref 550119WO patent application no. 2005,0443,02, Selective erbb2 inhibitor/anti-erbb antibody combinations in the treatment of cancer.
Ref 550178WO patent application no. 2014,1441,21, Classification and actionability indices for lung cancer.
Ref 550278Characterization 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.
Ref 550288Clinical pipeline report, company report or official report of AstraZeneca (2009).
Ref 550386Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
Ref 550422National Cancer Institute Drug Dictionary (drug id 596693).
Ref 550797Clinical pipeline report, company report or official report of Genentech (2009).
Ref 550963Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
Ref 551607Clinical pipeline report, company report or official report of Roche (2009).
Ref 551683Clinical pipeline report, company report or official report of Shionogi (2011).
Ref 551717Clinical pipeline report, company report or official report of Takeda (2009).
Ref 551787Clinical pipeline report, company report or official report of Zensun.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 889442Bispecific antibodies rise again. Nat Rev Drug Discov. 2014 Nov;13(11):799-801. doi: 10.1038/nrd4478.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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