Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT6EO5L)

• DTT Name: Erbb2 tyrosine kinase receptor (HER2)
• Synonyms: p185erbB2; Tyrosine kinase-type cell surface receptor HER2; Receptor tyrosine-protein kinase erbB-2; Proto-oncogene c-ErbB-2; Proto-oncogene Neu; NGL; NEU; Metastatic lymph node gene 19 protein; MLN19; MLN 19; HER2; CD340
• Gene Name: ERBB2
• DTT Type: Successful target; [1]
• BioChemical Class: Kinase
• UniProt ID: ERBB2_HUMAN
• TTD ID: T14597
• 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
• Function: Protein tyrosine kinase that is part of several cell surface receptor complexes, but that apparently needs a coreceptor for ligand binding. Essential component of a neuregulin-receptor complex, although neuregulins do not interact with it alone. GP30 is a potential ligand for this receptor. Regulates outgrowth and stabilization of peripheral microtubules (MTs). Upon ERBB2 activation, the MEMO1-RHOA-DIAPH1 signaling pathway elicits the phosphorylation and thus the inhibition of GSK3B at cell membrane. This prevents the phosphorylation of APC and CLASP2, allowing its association with the cell membrane. In turn, membrane-bound APC allows the localization of MACF1 to the cell membrane, which is required for microtubule capture and stabilization.
• KEGG Pathway:
  ErbB signaling pathway (hsa04012)
  Calcium signaling pathway (hsa04020)
  HIF-1 signaling pathway (hsa04066)
  Focal adhesion (hsa04510)
  Adherens junction (hsa04520)
  Pathways in cancer (hsa05200)
  Proteoglycans in cancer (hsa05205)
  MicroRNAs in cancer (hsa05206)
  Pancreatic cancer (hsa05212)
  Endometrial cancer (hsa05213)
  Prostate cancer (hsa05215)
  Bladder cancer (hsa05219)
  Non-small cell lung cancer (hsa05223)
  Central carbon metabolism in cancer (hsa05230)
• Reactome Pathway:
  PLCG1 events in ERBB2 signaling (R-HSA-1251932)
  PIP3 activates AKT signaling (R-HSA-1257604)
  GRB2 events in ERBB2 signaling (R-HSA-1963640)
  PI3K events in ERBB2 signaling (R-HSA-1963642)
  Constitutive Signaling by Aberrant PI3K in Cancer (R-HSA-2219530)
  Sema4D induced cell migration and growth-cone collapse (R-HSA-416572)
  RAF/MAP kinase cascade (R-HSA-5673001)
  SHC1 events in ERBB2 signaling (R-HSA-1250196)

Molecular Interaction Atlas (MIA) of This DTT

10 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BIBW 2992	DMTKD7Q	Non-small-cell lung cancer	2C25.Y	Approved	[2]
Dacomitinib	DMOH8VY	Non-small-cell lung cancer	2C25.Y	Approved	[3]
Lapatinib	DM3BH1Y	Breast cancer	2C60-2C65	Approved	[4]
Margetuximab	DMKEY6S	HER2-positive breast cancer	2C60-2C65	Approved	[5]
Masoprocol	DMMVNZ0	Prostate cancer	2C82.0	Approved	[6]
Merimepodib	DM0HS92	Breast cancer	2C60-2C65	Approved	[7]
NERATINIB MALEATE	DMEDU7B	HER2/NEU overexpressing breast cancer	2C60-2C65	Approved	[8]
Pertuzumab	DMHJV0X	Adrenal gland neoplasm		Approved	[9]
Trastuzumab	DMZQOUX	Breast cancer	2C60-2C65	Approved	[1]
Tucatinib	DMBESUA	HER2-positive breast cancer	2C60-2C65	Approved	[10]

74 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
HKI-272	DM6QOVN	Breast cancer	2C60-2C65	Phase 3	[11]
Nelipepimut S	DMDBY30	Non-hodgkin lymphoma	2B33.5	Phase 3	[12]
NeuVax	DMYTC4I	Breast cancer	2C60-2C65	Phase 3	[12]
PF-05280014	DM23BUP	Breast cancer	2C60-2C65	Phase 3	[13]
SYD985	DM0JC9L	Breast cancer	2C60-2C65	Phase 3	[14]
Taxol/Paraplatin/Herceptin	DML6GAN	Breast cancer	2C60-2C65	Phase 3	[15]
Trastuzumab-DM1	DMLB3I4	Breast cancer	2C60-2C65	Phase 3	[16]
Varlitinib	DMDG8Q3	Metastatic biliary tract neoplasms	2C14-2C17	Phase 2/3	[17]
Anti-CD3 and anti-Her2/neu bispecific antibody-armed activated T cells	DMPRIHK	Breast cancer	2C60-2C65	Phase 2	[18]
AZD8931	DMFLCW4	Breast cancer	2C60-2C65	Phase 2	[19]
BMS-599626	DMDPQV5	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]
CI-1033	DMSI8N3	Lymphoma	2A80-2A86	Phase 2	[11]
CP-724714	DMUJ0W7	Lymphoma	2A80-2A86	Phase 2	[11]
DN24-02	DM725UG	Colorectal cancer	2B91.Z	Phase 2	[20]
Ertumaxomab	DM5Z3VP	Breast cancer	2C60-2C65	Phase 2	[21]
HER-2 Protein AutoVac	DM8TOS0	Breast cancer	2C60-2C65	Phase 2	[22]
Her2-targeted autologous T-cell therapy	DMQTREC	Glioblastoma multiforme	2A00.0	Phase 2	[23]
HER2/neu peptide vaccine	DMISETH	Breast cancer	2C60-2C65	Phase 2	[24]
HM-78136B	DMZ3BER	HER2-positive breast cancer	2C60-2C65	Phase 2	[25]
KN026	DMNLH9W	Breast cancer	2C60-2C65	Phase 2	[26]
MCLA-128	DM0W3R7	Breast cancer	2C60-2C65	Phase 2	[27]
MGAH22	DMIXT2Y	Solid tumour/cancer	2A00-2F9Z	Phase 2	[28]
MM-111	DMO7MBS	Breast cancer	2C60-2C65	Phase 2	[29]
MRG002	DMJK8L1	Urothelial carcinoma	2C92.0	Phase 2	[30]
Tarloxotinib	DMA7ISF	Non-small-cell lung cancer	2C25.Y	Phase 2	[31]
Zenocutuzumab	DM1FLHH	Pancreatic cancer	2C10	Phase 2	[32]
A166	DMGTOIX	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[33]
ABY-025	DM31NJU	Bladder cancer	2C94	Phase 1/2	[34]
AGN-208397	DMHZUF8	Retina venous occlusion	9B74.1	Phase 1/2	[35]
Anti-HER2 CAR-T	DMQD6B9	Colorectal cancer	2B91.Z	Phase 1/2	[36]
AU105	DMPAZ3U	Recurrent glioblastoma	2A00.00	Phase 1/2	[37]
AVX901	DM7O29W	Breast cancer	2C60-2C65	Phase 1/2	[38]
BDTX-189	DMODTX5	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[39]
CART-HER-2	DMMTDK1	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[40]
HER-2-targeting CAR T Cells	DM1U6VX	Breast cancer	2C60-2C65	Phase 1/2	[41]
ISB 1302	DM1WD8F	HER2-positive breast cancer	2C60-2C65	Phase 1/2	[42]
Sym013	DMZM6I2	Epithelial ovarian cancer	2B5D	Phase 1/2	[27]
TAS-0728	DM13AH8	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[43]
Zenocutuzomab	DMMQGPE	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[44]
S-222611	DMQGH76	Malignant solid tumour	2C10-2F32	Phase 1b	[45]
ACE1702	DMHI7DX	Aggressive cancer	2A00-2F9Z	Phase 1	[46]
AIP-303	DMHCBI0	Breast cancer	2C60-2C65	Phase 1	[47]
ARRY-380	DMCNV0M	Solid tumour/cancer	2A00-2F9Z	Phase 1	[48]
BAY 2701439	DM98EP5	Solid tumour/cancer	2A00-2F9Z	Phase 1	[49]
BB-1701	DMOAK6T	Aggressive cancer	2A00-2F9Z	Phase 1	[50]
CAR-T cells targeting HER2	DMLI5VG	Pancreatic cancer	2C10	Phase 1	[51]
Cipatinib	DMJLNEF	Solid tumour/cancer	2A00-2F9Z	Phase 1	[17]
CUDC-101	DM9ZOMD	Solid tumour/cancer	2A00-2F9Z	Phase 1	[52]
DZD1516	DMEQY4Z	HER2-positive breast cancer	2C60-2C65	Phase 1	[53]
GBR1302	DM52O7W	Solid tumour/cancer	2A00-2F9Z	Phase 1	[54]
GQ1001	DMFA2XQ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[55]
HER2-CAR T Cells	DMZXDBN	Malignant neoplasm	2A00-2F9Z	Phase 1	[56]
HER2-specific CAR T cell	DMJKBWO	Atypical teratoid/rhabdoid tumour	2A00.1Y	Phase 1	[57]
HER2-specific T cells	DM7UJ6E	Recurrent glioblastoma	2A00.00	Phase 1	[58]
HER2p63-71 peptide vaccine	DMJ52F9	Solid tumour/cancer	2A00-2F9Z	Phase 1	[59]
JNJ-26483327	DMSQ3AZ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[60]
M802	DM132EG	Solid tumour/cancer	2A00-2F9Z	Phase 1	[61]
MB-103	DMS0P5O	Glioblastoma multiforme	2A00.0	Phase 1	[62]
MBS301	DM85AXS	Solid tumour/cancer	2A00-2F9Z	Phase 1	[63]
MEDI4276	DMNI60O	Solid tumour/cancer	2A00-2F9Z	Phase 1	[27]
MM-302	DMYSJTR	Breast cancer	2C60-2C65	Phase 1	[64]
MT-5111	DM5SN0A	Solid tumour/cancer	2A00-2F9Z	Phase 1	[65]
MVA HER-2 AutoVac	DM3JUXW	Breast cancer	2C60-2C65	Phase 1	[66]
NJH395	DMSENTW	HER2-positive metastatic breast cancer	2C60-2C65	Phase 1	[67]
Recombinant human Erbb3 fragment therapeutic tumor vaccine	DMK9Y71	Solid tumour/cancer	2A00-2F9Z	Phase 1	[68]
Runimotamab	DML6BK5	Breast cancer	2C60-2C65	Phase 1	[69]
SAR443216	DMUQNG6	Gastric cancer	2B72	Phase 1	[70]
SBT6050	DMHBD3T	Solid tumour/cancer	2A00-2F9Z	Phase 1	[71]
TAK-285	DM6KOBZ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[72]
TrasGEX	DMMRDUN	Solid tumour/cancer	2A00-2F9Z	Phase 1	[73]
TT16	DM5YL4N	Aggressive cancer	2A00-2F9Z	Phase 1	[74]
VM-206	DMB3I04	Solid tumour/cancer	2A00-2F9Z	Phase 1	[75]
Zemab	DM2S04R	Solid tumour/cancer	2A00-2F9Z	Phase 1	[76]
ZW49	DMAU8L9	Solid tumour/cancer	2A00-2F9Z	Phase 1	[77]

3 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Her-2-Bi-armed ATC	DM5JZW2	Breast cancer	2C60-2C65	Discontinued in Phase 2	[78]
TAK165	DMBE5OF	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[11]
GW-974	DMPLYHU	Breast cancer	2C60-2C65	Terminated	[80]

1 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
227Th-labelled HER2-TTC	DM1O2C3	Solid tumour/cancer	2A00-2F9Z	Preclinical	[79]

6 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(1-Benzyl-1H-indazol-5-yl)-quinazolin-4-yl-amine	DMNIP7J	Discovery agent	N.A.	Investigative	[81]
(1-Benzyl-1H-indol-5-yl)-quinazolin-4-yl-amine	DM0SCW9	Discovery agent	N.A.	Investigative	[81]
PF 5208766	DMY45K1	Discovery agent	N.A.	Investigative	[82]
Redoxal	DM2S496	Discovery agent	N.A.	Investigative	[83]
TA1-RTA	DMP2016	Discovery agent	N.A.	Investigative	[84]
YH012	DMG3WBJ	Aggressive cancer	2A00-2F9Z	Investigative	[85]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Bladder cancer	2C82	Bladder tissue	5.67E-03	-1.26	-2.05
Gastric cancer	2C82	Gastric tissue	2.78E-03	0.59	4.11
Lung cancer	2C82	Lung tissue	7.14E-04	-0.13	-0.19
Breast cancer	2C82	Breast tissue	3.50E-77	0.49	1.12
Glioma	2C82	Brainstem tissue	1.98E-01	0.21	1.79
Glioma	2C82	White matter	2.06E-01	-0.15	-0.94

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