Target Information

Target General Infomation
Target ID
T86350
Former ID
TTDR01265
Target Name
Receptor protein-tyrosine kinase erbB-3
Gene Name
ERBB3
Synonyms
C-erbB-3 protein; C-erbB3; Tyrosine kinase-type cell surface receptor HER3; ERBB3
Target Type
Clinical Trial
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.
BioChemical Class
Kinase
UniProt ID
P21860
EC Number
EC 2.7.10.1
Sequence
MRANDALQVLGLLFSLARGSEVGNSQAVCPGTLNGLSVTGDAENQYQTLYKLYERCEVVM
GNLEIVLTGHNADLSFLQWIREVTGYVLVAMNEFSTLPLPNLRVVRGTQVYDGKFAIFVM
LNYNTNSSHALRQLRLTQLTEILSGGVYIEKNDKLCHMDTIDWRDIVRDRDAEIVVKDNG
RSCPPCHEVCKGRCWGPGSEDCQTLTKTICAPQCNGHCFGPNPNQCCHDECAGGCSGPQD
TDCFACRHFNDSGACVPRCPQPLVYNKLTFQLEPNPHTKYQYGGVCVASCPHNFVVDQTS
CVRACPPDKMEVDKNGLKMCEPCGGLCPKACEGTGSGSRFQTVDSSNIDGFVNCTKILGN
LDFLITGLNGDPWHKIPALDPEKLNVFRTVREITGYLNIQSWPPHMHNFSVFSNLTTIGG
RSLYNRGFSLLIMKNLNVTSLGFRSLKEISAGRIYISANRQLCYHHSLNWTKVLRGPTEE
RLDIKHNRPRRDCVAEGKVCDPLCSSGGCWGPGPGQCLSCRNYSRGGVCVTHCNFLNGEP
REFAHEAECFSCHPECQPMEGTATCNGSGSDTCAQCAHFRDGPHCVSSCPHGVLGAKGPI
YKYPDVQNECRPCHENCTQGCKGPELQDCLGQTLVLIGKTHLTMALTVIAGLVVIFMMLG
GTFLYWRGRRIQNKRAMRRYLERGESIEPLDPSEKANKVLARIFKETELRKLKVLGSGVF
GTVHKGVWIPEGESIKIPVCIKVIEDKSGRQSFQAVTDHMLAIGSLDHAHIVRLLGLCPG
SSLQLVTQYLPLGSLLDHVRQHRGALGPQLLLNWGVQIAKGMYYLEEHGMVHRNLAARNV
LLKSPSQVQVADFGVADLLPPDDKQLLYSEAKTPIKWMALESIHFGKYTHQSDVWSYGVT
VWELMTFGAEPYAGLRLAEVPDLLEKGERLAQPQICTIDVYMVMVKCWMIDENIRPTFKE
LANEFTRMARDPPRYLVIKRESGPGIAPGPEPHGLTNKKLEEVELEPELDLDLDLEAEED
NLATTTLGSALSLPVGTLNRPRGSQSLLSPSSGYMPMNQGNLGESCQESAVSGSSERCPR
PVSLHPMPRGCLASESSEGHVTGSEAELQEKVSMCRSRSRSRSPRPRGDSAYHSQRHSLL
TPVTPLSPPGLEEEDVNGYVMPDTHLKGTPSSREGTLSSVGLSSVLGTEEEDEDEEYEYM
NRRRRHSPPHPPRPSSLEELGYEYMDVGSDLSASLGSTQSCPLHPVPIMPTAGTTPDEDY
EYMNRQRDGGGPGGDYAAMGACPASEQGYEEMRAFQGPGHQAPHVHYARLKTLRSLEATD
SAFDNPDYWHSRLFPKANAQRT
Drugs and Mode of Action
Drug(s) Elisidepsin Drug Info Phase 2 Psoriasis [1]
MEHD-7945A Drug Info Phase 2 Solid tumours [2]
MEHD7945A Drug Info Phase 2 Colorectal cancer; Head and neck cancer [2], [3]
MM-121 Drug Info Phase 2 Breast cancer [4]
MM-141 Drug Info Phase 2 Cancer [5]
AMG888/U3-1287 Drug Info Phase 1/2 Non-small cell lung cancer [6]
LJM716 Drug Info Phase 1/2 Breast cancer [7]
Anti-HER3/EGFR DAF Drug Info Phase 1 Metastatic epithelial tumors [8]
AV-203 Drug Info Phase 1 Cancer [9]
Drug 2849330 Drug Info Phase 1 Cancer [10]
GSK2849330 Drug Info Phase 1 Cancer [10]
KTN3379 Drug Info Phase 1 Late-stage solid tumors [11]
MM-151 Drug Info Phase 1 Solid tumours [12]
Patritumab Drug Info Phase 1 Non-small cell lung cancer [13]
Recombinant human Erbb3 fragment therapeutic tumor vaccine Drug Info Phase 1 Cancer [14]
REGN1400 Drug Info Phase 1 Cancer [15]
RG7116 Drug Info Phase 1 Solid tumours [16]
Modulator AMG888/U3-1287 Drug Info [17]
Anti-HER3/EGFR DAF Drug Info
MEHD-7945A Drug Info
MEHD7945A Drug Info [18]
MM-121 Drug Info
MM-141 Drug Info [19]
MM-151 Drug Info [19]
RG7116 Drug Info [20]
SYM-011 Drug Info [17]
Inhibitor Elisidepsin Drug Info [21]
Soluble ErbB3 theragnostics Drug Info [17]
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 1First-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 2ClinicalTrials.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 3ClinicalTrials.gov (NCT01577173) A Study of MEHD7945A Versus Cetuximab in Patients With Recurrent/Metastatic Squamous Cell Carcinoma of The Head And Neck
REF 4ClinicalTrials.gov (NCT01447706) A Study of MM-121 With Paclitaxel in Platinum Resistant/ Refractory Advanced Ovarian Cancers. U.S. National Institutes of Health.
REF 5ClinicalTrials.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 6ClinicalTrials.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 7ClinicalTrials.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 8Clinical pipeline report, company report or official report of Genentech (2011).
REF 9ClinicalTrials.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 10ClinicalTrials.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 11ClinicalTrials.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 12Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035447)
REF 13ClinicalTrials.gov (NCT01957280) Study to Assess Pharmacokinetics, Immunogenicity and Safety/Tolerability of Patritumab (U3-1287). U.S. National Institutes of Health.
REF 14Clinical pipeline report, company report or official report of Zensun.
REF 15Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036915)
REF 16Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035594)
REF 17(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).
REF 18Bispecific antibodies rise again. Nat Rev Drug Discov. 2014 Nov;13(11):799-801. doi: 10.1038/nrd4478.
REF 19MM-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 20RG7116, 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 21Molecular 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.

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