Id: acc2519
Group: 2sens
Protein: HER2
Gene Symbol: ERBB2
Protein Id: P04626
Protein Name: ERBB2_HUMAN
PTM: ubiquitination
Site: unclear
Site Sequence:
Disease Category: Cancer
Disease: Breast Cancer
Disease Subtype: ductal carcinoma
Disease Cellline: BT474
Disease Info:
Drug: peptide p37
Drug Info: -
Effect: modulate
Effect Info: "Promote HER2 ubiquitination and subsequent lysosomal degradation, leading to decreased cell growth and increased apoptosis, and inhibit tumor growth in vivo."
Note:
Score: 4.0
Pubmed(PMID): 25898135
Sentence Index:
Sentence:

Sequence & Structure:

MELAALCRWGLLLALLPPGAASTQVCTGTDMKLRLPASPETHLDMLRHLYQGCQVVQGNLELTYLPTNASLSFLQDIQEVQGYVLIAHNQVRQVPLQRLRIVRGTQLFEDNYALAVLDNGDPLNNTTPVTGASPGGLRELQLRSLTEILKGGVLIQRNPQLCYQDTILWKDIFHKNNQLALTLIDTNRSRACHPCSPMCKGSRCWGESSEDCQSLTRTVCAGGCARCKGPLPTDCCHEQCAAGCTGPKHSDCLACLHFNHSGICELHCPALVTYNTDTFESMPNPEGRYTFGASCVTACPYNYLSTDVGSCTLVCPLHNQEVTAEDGTQRCEKCSKPCARVCYGLGMEHLREVRAVTSANIQEFAGCKKIFGSLAFLPESFDGDPASNTAPLQPEQLQVFETLEEITGYLYISAWPDSLPDLSVFQNLQVIRGRILHNGAYSLTLQGLGISWLGLRSLRELGSGLALIHHNTHLCFVHTVPWDQLFRNPHQALLHTANRPEDECVGEGLACHQLCARGHCWGPGPTQCVNCSQFLRGQECVEECRVLQGLPREYVNARHCLPCHPECQPQNGSVTCFGPEADQCVACAHYKDPPFCVARCPSGVKPDLSYMPIWKFPDEEGACQPCPINCTHSCVDLDDKGCPAEQRASPLTSIISAVVGILLVVVLGVVFGILIKRRQQKIRKYTMRRLLQETELVEPLTPSGAMPNQAQMRILKETELRKVKVLGSGAFGTVYKGIWIPDGENVKIPVAIKVLRENTSPKANKEILDEAYVMAGVGSPYVSRLLGICLTSTVQLVTQLMPYGCLLDHVRENRGRLGSQDLLNWCMQIAKGMSYLEDVRLVHRDLAARNVLVKSPNHVKITDFGLARLLDIDETEYHADGGKVPIKWMALESILRRRFTHQSDVWSYGVTVWELMTFGAKPYDGIPAREIPDLLEKGERLPQPPICTIDVYMIMVKCWMIDSECRPRFRELVSEFSRMARDPQRFVVIQNEDLGPASPLDSTFYRSLLEDDDMGDLVDAEEYLVPQQGFFCPDPAPGAGGMVHHRHRSSSTRSGGGDLTLGLEPSEEEAPRSPLAPSEGAGSDVFDGDLGMGAAKGLQSLPTHDPSPLQRYSEDPTVPLPSETDGYVAPLTCSPQPEYVNQPDVRPQPPSPREGPLPAARPAGATLERPKTLSPGKNGVVKDVFAFGGAVENPEYLTPQGGAAPQPHPPPAFSPAFDNLYYWDQDPPERGAPPSTFKGTPTAENPEYLGLDVPV

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
ERBB2 LAPATINIB DITOSYLATE Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - breast carcinoma FDA
ERBB2 TRASTUZUMAB EMTANSINE Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - breast carcinoma DailyMed
ERBB2 NERATINIB MALEATE Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - breast carcinoma FDA
ERBB2 TRASTUZUMAB Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - breast carcinoma DailyMed
ERBB2 PERTUZUMAB Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - breast carcinoma DailyMed
ERBB2 TRASTUZUMAB EMTANSINE Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - neoplasm ATC
ERBB2 PERTUZUMAB Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - neoplasm ATC
ERBB2 TRASTUZUMAB Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - neoplasm ATC
ERBB2 DACOMITINIB Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - neoplasm ATC
ERBB2 VANDETANIB Epidermal growth factor receptor inhibitor 4 - neoplasm ATC
ERBB2 MASOPROCOL Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - neoplasm ATC
ERBB2 TUCATINIB Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - neoplasm ATC
ERBB2 TRASTUZUMAB DERUXTECAN Receptor protein-tyrosine kinase erbB-2 binding agent 4 - neoplasm ATC
ERBB2 MARGETUXIMAB Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - neoplasm ATC
ERBB2 VANDETANIB Epidermal growth factor receptor inhibitor 4 - thyroid carcinoma DailyMed
ERBB2 AFATINIB DIMALEATE Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - non-small cell lung carcinoma DailyMed
ERBB2 AFATINIB DIMALEATE Receptor protein-tyrosine kinase erbB-2 inhibitor 4 Not yet recruiting non-small cell lung carcinoma ClinicalTrials
ERBB2 DACOMITINIB Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - non-small cell lung carcinoma EMA
FDA
ERBB2 VANDETANIB Epidermal growth factor receptor inhibitor 4 - thyroid neoplasm EMA
ERBB2 TUCATINIB Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - breast neoplasm EMA
ERBB2 TRASTUZUMAB Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - breast neoplasm EMA
ERBB2 TRASTUZUMAB DERUXTECAN Receptor protein-tyrosine kinase erbB-2 binding agent 4 - breast neoplasm EMA
ERBB2 PERTUZUMAB Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - breast neoplasm EMA
ERBB2 TRASTUZUMAB EMTANSINE Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - breast neoplasm EMA
ERBB2 TRASTUZUMAB Receptor protein-tyrosine kinase erbB-2 inhibitor 4 - stomach neoplasm EMA

Note: Only show clinically investigational or approved drugs with protein targets.

Protein Tractability:

source: Open Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC

No data.

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
- - P Colon cancer/carcinoma Phosphorylation 23739740
- - U Breast cancer/tumor/carcinoma Phosphorylation 24285542
- - U Breast cancer/tumor/carcinoma Phosphorylation 23794518
- - U Oral squamous cell carcinoma Phosphorylation 35415372

State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.

PTM-Drug Perturbation Response:

source: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: