Target Information

Target General Infomation
Target ID
T96788
Former ID
TTDR01361
Target Name
mRNA of HER2
Gene Name
ERBB2
Synonyms
CD340 (mRNA); MLN 19 (mRNA); Metastatic lymph node gene 19 protein (mRNA); Proto-oncogene Neu (mRNA); Proto-oncogene c-ErbB-2 (mRNA); Tyrosine kinase-type cell surface receptor HER2 (mRNA); p185erbB2 (mRNA); ERBB2
Target Type
Clinical Trial
Disease Breast cancer [ICD9: 174, 175; ICD10: C50]
Chronic pain [ICD9: 338.2,780; ICD10: R52.1-R52.2, G89]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Function
In the nucleus is involved in transcriptional 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. Involvedin the transcription of rRNA genes by RNA Pol I and enhances protein synthesis and cell growth.
BioChemical Class
Kinase
Target Validation
T96788
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
Drugs and Mode of Action
Drug(s) HKI-272 Drug Info Phase 3 Breast cancer [548009]
BMS-690514 Drug Info Phase 2 Chronic pain [528940]
Inhibitor (1-Benzyl-1H-indol-5-yl)-quinazolin-4-yl-amine Drug Info [526072]
17-allylamino-17-desmethoxy-geldanamycin Drug Info [529815]
3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione Drug Info [528032]
3,4-diphenyl-1H-pyrrole-2,5-dione Drug Info [528032]
3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione Drug Info [528032]
3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione Drug Info [528032]
4-(3-phenoxylphenyl)-5-cyano-2H-1,2,3-triazole Drug Info [528580]
4-(4-bromophenyl)-5-cyano-2H-1,2,3-triazole Drug Info [528580]
4-(4-chlorophenyl)-5-cyano-2H-1,2,3-triazole Drug Info [528580]
4-(4-isopropylphenyl)-5-cyano-2H-1,2,3-triazole Drug Info [528580]
4-(Bis(2-chloroethyl)amino)-N-p-tolylbenzamide Drug Info [530574]
4557W Drug Info [526072]
AG-213 Drug Info [529134]
BMS-536924 Drug Info [527711]
BMS-690514 Drug Info [530732]
CL-387785 Drug Info [528037]
compound 38 Drug Info [532836]
Geldanamycin-estradiol hybrid Drug Info [525501]
HDS-029 Drug Info [528037]
HKI-272 Drug Info [529214]
N-(4-m-Tolylamino-quinazolin-6-yl)-acrylamide Drug Info [525502]
PD-168393 Drug Info [525502]
PNT-500 Drug Info [543538]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP 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
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 528940A novel epidermal growth factor receptor inhibitor promotes apoptosis in non-small cell lung cancer cells resistant to erlotinib. Cancer Res. 2007 Jul 1;67(13):6253-62.
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 525501Bioorg Med Chem Lett. 1999 May 3;9(9):1233-8.Synthesis and evaluation of geldanamycin-estradiol hybrids.
Ref 525502J Med Chem. 1999 May 20;42(10):1803-15.Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding siteof the epidermal growth factor receptor.
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 527711J Med Chem. 2005 Sep 8;48(18):5639-43.Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.
Ref 528032J Med Chem. 2006 Feb 23;49(4):1271-81.Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors.
Ref 528037J Med Chem. 2006 Feb 23;49(4):1475-85.Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.
Ref 528580Bioorg Med Chem. 2007 Feb 1;15(3):1533-8. Epub 2006 Dec 15.Synthesis and biological evaluation of 4-aryl-5-cyano-2H-1,2,3-triazoles as inhibitor of HER2 tyrosine kinase.
Ref 529134Eur J Med Chem. 2008 Jul;43(7):1478-88. Epub 2007 Sep 29.Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors.
Ref 529214Proc Natl Acad Sci U S A. 2007 Dec 11;104(50):19936-41. Epub 2007 Dec 6.Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
Ref 529815Bioorg Med Chem. 2009 Mar 15;17(6):2225-35. Epub 2008 Nov 6.Discovery and development of heat shock protein 90 inhibitors.
Ref 530574Bioorg Med Chem. 2010 Jan 15;18(2):880-6. Epub 2009 Nov 22.Synthesis, biological evaluation and molecular docking studies of amide-coupled benzoic nitrogen mustard derivatives as potential antitumoragents.
Ref 530732Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93.
Ref 532836Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. J Med Chem. 2014 Jun 26;57(12):5112-28.
Ref 543538(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: 2019).
Ref 549610US patent application no. 5,968,748, Antisense oligonucleotide modulation of human HER-2 expression.

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