Target Information
Target General Infomation | |||||
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Target ID |
T86350
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Former ID |
TTDR01265
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Target Name |
Receptor protein-tyrosine kinase erbB-3
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Gene Name |
ERBB3
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Synonyms |
C-erbB-3 protein; C-erbB3; Tyrosine kinase-type cell surface receptor HER3; ERBB3
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Target Type |
Clinical Trial
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Disease | Breast cancer [ICD9: 174, 175; ICD10: C50] | ||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Colorectal cancer; Head and neck cancer [ICD9: 140-149, 153, 154; ICD10: C18-C21, C07-C14, C32-C33] | |||||
Late-stage solid tumors [ICD9: 140-199, 210-229; ICD10: C00-C75, C7A, C7B, D10-D36, D3A] | |||||
Metastatic epithelial tumors [ICD9: 140-199; ICD10: C00-C75, C7A, C7B] | |||||
Non-small cell lung cancer [ICD10: C33-C34] | |||||
Psoriasis [ICD9: 696; ICD10: L40] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Function |
Binds and is activated by neuregulins and NTAK. May also be activated by CSPG5.
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BioChemical Class |
Kinase
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UniProt ID | |||||
EC Number |
EC 2.7.10.1
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Sequence |
MRANDALQVLGLLFSLARGSEVGNSQAVCPGTLNGLSVTGDAENQYQTLYKLYERCEVVM
GNLEIVLTGHNADLSFLQWIREVTGYVLVAMNEFSTLPLPNLRVVRGTQVYDGKFAIFVM LNYNTNSSHALRQLRLTQLTEILSGGVYIEKNDKLCHMDTIDWRDIVRDRDAEIVVKDNG RSCPPCHEVCKGRCWGPGSEDCQTLTKTICAPQCNGHCFGPNPNQCCHDECAGGCSGPQD TDCFACRHFNDSGACVPRCPQPLVYNKLTFQLEPNPHTKYQYGGVCVASCPHNFVVDQTS CVRACPPDKMEVDKNGLKMCEPCGGLCPKACEGTGSGSRFQTVDSSNIDGFVNCTKILGN LDFLITGLNGDPWHKIPALDPEKLNVFRTVREITGYLNIQSWPPHMHNFSVFSNLTTIGG RSLYNRGFSLLIMKNLNVTSLGFRSLKEISAGRIYISANRQLCYHHSLNWTKVLRGPTEE RLDIKHNRPRRDCVAEGKVCDPLCSSGGCWGPGPGQCLSCRNYSRGGVCVTHCNFLNGEP REFAHEAECFSCHPECQPMEGTATCNGSGSDTCAQCAHFRDGPHCVSSCPHGVLGAKGPI YKYPDVQNECRPCHENCTQGCKGPELQDCLGQTLVLIGKTHLTMALTVIAGLVVIFMMLG GTFLYWRGRRIQNKRAMRRYLERGESIEPLDPSEKANKVLARIFKETELRKLKVLGSGVF GTVHKGVWIPEGESIKIPVCIKVIEDKSGRQSFQAVTDHMLAIGSLDHAHIVRLLGLCPG SSLQLVTQYLPLGSLLDHVRQHRGALGPQLLLNWGVQIAKGMYYLEEHGMVHRNLAARNV LLKSPSQVQVADFGVADLLPPDDKQLLYSEAKTPIKWMALESIHFGKYTHQSDVWSYGVT VWELMTFGAEPYAGLRLAEVPDLLEKGERLAQPQICTIDVYMVMVKCWMIDENIRPTFKE LANEFTRMARDPPRYLVIKRESGPGIAPGPEPHGLTNKKLEEVELEPELDLDLDLEAEED NLATTTLGSALSLPVGTLNRPRGSQSLLSPSSGYMPMNQGNLGESCQESAVSGSSERCPR PVSLHPMPRGCLASESSEGHVTGSEAELQEKVSMCRSRSRSRSPRPRGDSAYHSQRHSLL TPVTPLSPPGLEEEDVNGYVMPDTHLKGTPSSREGTLSSVGLSSVLGTEEEDEDEEYEYM NRRRRHSPPHPPRPSSLEELGYEYMDVGSDLSASLGSTQSCPLHPVPIMPTAGTTPDEDY EYMNRQRDGGGPGGDYAAMGACPASEQGYEEMRAFQGPGHQAPHVHYARLKTLRSLEATD SAFDNPDYWHSRLFPKANAQRT |
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Drugs and Mode of Action | |||||
Drug(s) | Elisidepsin | Drug Info | Phase 2 | Psoriasis | [533234] |
MEHD-7945A | Drug Info | Phase 2 | Solid tumours | [523994] | |
MEHD7945A | Drug Info | Phase 2 | Colorectal cancer; Head and neck cancer | [523994], [889373] | |
MM-121 | Drug Info | Phase 2 | Breast cancer | [523649] | |
MM-141 | Drug Info | Phase 2 | Cancer | [525130] | |
AMG888/U3-1287 | Drug Info | Phase 1/2 | Non-small cell lung cancer | [523187] | |
LJM716 | Drug Info | Phase 1/2 | Breast cancer | [524764] | |
Anti-HER3/EGFR DAF | Drug Info | Phase 1 | Metastatic epithelial tumors | [550794] | |
AV-203 | Drug Info | Phase 1 | Cancer | [523911] | |
Drug 2849330 | Drug Info | Phase 1 | Cancer | [524480] | |
GSK2849330 | Drug Info | Phase 1 | Cancer | [524480] | |
KTN3379 | Drug Info | Phase 1 | Late-stage solid tumors | [524573] | |
MM-151 | Drug Info | Phase 1 | Solid tumours | [549340] | |
Patritumab | Drug Info | Phase 1 | Non-small cell lung cancer | [524459] | |
Recombinant human Erbb3 fragment therapeutic tumor vaccine | Drug Info | Phase 1 | Cancer | [551788] | |
REGN1400 | Drug Info | Phase 1 | Cancer | [549420] | |
RG7116 | Drug Info | Phase 1 | Solid tumours | [549350] | |
Modulator | AMG888/U3-1287 | Drug Info | [543486] | ||
Anti-HER3/EGFR DAF | Drug Info | ||||
MEHD-7945A | Drug Info | ||||
MEHD7945A | Drug Info | [889442] | |||
MM-121 | Drug Info | ||||
MM-141 | Drug Info | [532567] | |||
MM-151 | Drug Info | [532567] | |||
RG7116 | Drug Info | [532402] | |||
SYM-011 | Drug Info | [543486] | |||
Inhibitor | Elisidepsin | Drug Info | [530057] | ||
Soluble ErbB3 theragnostics | Drug Info | [543486] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | ErbB signaling pathway | ||||
Calcium signaling pathway | |||||
Endocytosis | |||||
Proteoglycans in cancer | |||||
MicroRNAs in cancer | |||||
NetPath Pathway | TNFalpha Signaling Pathway | ||||
PANTHER Pathway | Cadherin signaling pathway | ||||
EGF receptor signaling pathway | |||||
Pathway Interaction Database | ErbB2/ErbB3 signaling events | ||||
ErbB receptor signaling network | |||||
a6b1 and a6b4 Integrin signaling | |||||
WikiPathways | ErbB Signaling Pathway | ||||
Apoptosis-related network due to altered Notch3 in ovarian cancer | |||||
Signaling Pathways in Glioblastoma | |||||
miR-targeted genes in muscle cell - TarBase | |||||
Heart Development | |||||
References | |||||
Ref 523187 | ClinicalTrials.gov (NCT01211483) Study of Erlotinib With or Without Investigational Drug (U3-1287) in Subjects With Advanced Non-small Cell Lung Cancer. U.S. National Institutes of Health. | ||||
Ref 523649 | ClinicalTrials.gov (NCT01447706) A Study of MM-121 With Paclitaxel in Platinum Resistant/ Refractory Advanced Ovarian Cancers. U.S. National Institutes of Health. | ||||
Ref 523911 | ClinicalTrials.gov (NCT01603979) A Phase 1 Dose Escalation Study of AV-203, an ERBB3 Inhibitory Antibody, in Subjects With Advanced Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 523994 | ClinicalTrials.gov (NCT01652482) A Study of MEHD7945A + FOLFIRI Versus Cetuximab + FOLFIRI in Second Line in Patients With KRAS Wild-Type Metastatic Colorectal Cancer. U.S. National Institutes of Health. | ||||
Ref 524459 | ClinicalTrials.gov (NCT01957280) Study to Assess Pharmacokinetics, Immunogenicity and Safety/Tolerability of Patritumab (U3-1287). U.S. National Institutes of Health. | ||||
Ref 524480 | ClinicalTrials.gov (NCT01966445) Dose Escalation Study to Investigate the Safety, Pharmacokinetics, and Pharmacodynamics of GSK2849330 in Subjects With Advanced Her3-Positive Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 524573 | ClinicalTrials.gov (NCT02014909) A Phase 1 Study to Evaluate the Safety and Pharmacokinetics of KTN3379 in Adult Subjects With Advanced Tumors. U.S. National Institutes of Health. | ||||
Ref 524764 | ClinicalTrials.gov (NCT02143622) Study of Efficacy and Safety of LJM716 and Cetuximab in Head and Neck Squamous Cell Carcinoma Patients. U.S. National Institutes of Health. | ||||
Ref 525130 | ClinicalTrials.gov (NCT02399137) A Phase 2 Study of MM-141 Plus Nab-paclitaxel and Gemcitabine in Front-line Metastatic Pancreatic Cancer. U.S. National Institutes of Health. | ||||
Ref 533234 | First-in-human, phase I study of elisidepsin (PM02734) administered as a 30-min or as a 3-hour intravenous infusion every three weeks in patients with advanced solid tumors. Invest New Drugs. 2015 Aug;33(4):901-10. | ||||
Ref 549340 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035447) | ||||
Ref 549350 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035594) | ||||
Ref 530057 | Molecular pharmacodynamics of PM02734 (elisidepsin) as single agent and in combination with erlotinib; synergistic activity in human non-small cell lung cancer cell lines and xenograft models. Eur J Cancer. 2009 Jul;45(10):1855-64. | ||||
Ref 531635 | Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36. | ||||
Ref 532402 | RG7116, a therapeutic antibody that binds the inactive HER3 receptor and is optimized for immune effector activation. Cancer Res. 2013 Aug 15;73(16):5183-94. | ||||
Ref 532451 | An antibody that locks HER3 in the inactive conformation inhibits tumor growth driven by HER2 or neuregulin. Cancer Res. 2013 Oct 1;73(19):6024-35. | ||||
Ref 532567 | MM-141, an IGF-IR- and ErbB3-directed bispecific antibody, overcomes network adaptations that limit activity of IGF-IR inhibitors. Mol Cancer Ther. 2014 Feb;13(2):410-25. | ||||
Ref 532632 | Phase 1 and dose-finding study of patritumab (U3-1287), a human monoclonal antibody targeting HER3, in Japanese patients with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Mar;73(3):511-6. | ||||
Ref 533093 | Neuregulin 1 expression is a predictive biomarker for response to AV-203, an ERBB3 inhibitory antibody, in human tumor models. Clin Cancer Res. 2015 Mar 1;21(5):1106-14. | ||||
Ref 543486 | (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. (Target id: 1798). |
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