Id: acc0808
Group: 2sens
Protein: HER3
Gene Symbol: ERBB3
Protein Id: P21860
Protein Name: ERBB3_HUMAN
PTM: phosphorylation
Site: Tyr1289
Site Sequence: GACPASEQGYEEMRAFQGPGH
Disease Category: Cancer
Disease: Breast Cancer
Disease Subtype:
Disease Cellline: BT474c
Disease Info:
Drug: AZD5363
Drug Info: "Capivasertib (AZD5363) is an orally active pan-AKT kinase inhibitor that inhibits Akt1, Akt2, and Akt3 with IC50 values of 3, 7, and 7 nM, respectively."
Effect: inhibit
Effect Info: "The addition of AZD8931 blocked the HER2/HER3 phosphorylation induced by AZD5363, leading to the concomitant inhibition of the PI3K/AKT/mTOR and ERK signaling pathways and the induction of apoptosis, thereby enhancing the activity of AZD5363 in HER2-amplified breast cancer cells."
Note:
Score: 5.0
Pubmed(PMID): 26095475
Sentence Index:
Sentence:

Sequence & Structure:

MRANDALQVLGLLFSLARGSEVGNSQAVCPGTLNGLSVTGDAENQYQTLYKLYERCEVVMGNLEIVLTGHNADLSFLQWIREVTGYVLVAMNEFSTLPLPNLRVVRGTQVYDGKFAIFVMLNYNTNSSHALRQLRLTQLTEILSGGVYIEKNDKLCHMDTIDWRDIVRDRDAEIVVKDNGRSCPPCHEVCKGRCWGPGSEDCQTLTKTICAPQCNGHCFGPNPNQCCHDECAGGCSGPQDTDCFACRHFNDSGACVPRCPQPLVYNKLTFQLEPNPHTKYQYGGVCVASCPHNFVVDQTSCVRACPPDKMEVDKNGLKMCEPCGGLCPKACEGTGSGSRFQTVDSSNIDGFVNCTKILGNLDFLITGLNGDPWHKIPALDPEKLNVFRTVREITGYLNIQSWPPHMHNFSVFSNLTTIGGRSLYNRGFSLLIMKNLNVTSLGFRSLKEISAGRIYISANRQLCYHHSLNWTKVLRGPTEERLDIKHNRPRRDCVAEGKVCDPLCSSGGCWGPGPGQCLSCRNYSRGGVCVTHCNFLNGEPREFAHEAECFSCHPECQPMEGTATCNGSGSDTCAQCAHFRDGPHCVSSCPHGVLGAKGPIYKYPDVQNECRPCHENCTQGCKGPELQDCLGQTLVLIGKTHLTMALTVIAGLVVIFMMLGGTFLYWRGRRIQNKRAMRRYLERGESIEPLDPSEKANKVLARIFKETELRKLKVLGSGVFGTVHKGVWIPEGESIKIPVCIKVIEDKSGRQSFQAVTDHMLAIGSLDHAHIVRLLGLCPGSSLQLVTQYLPLGSLLDHVRQHRGALGPQLLLNWGVQIAKGMYYLEEHGMVHRNLAARNVLLKSPSQVQVADFGVADLLPPDDKQLLYSEAKTPIKWMALESIHFGKYTHQSDVWSYGVTVWELMTFGAEPYAGLRLAEVPDLLEKGERLAQPQICTIDVYMVMVKCWMIDENIRPTFKELANEFTRMARDPPRYLVIKRESGPGIAPGPEPHGLTNKKLEEVELEPELDLDLDLEAEEDNLATTTLGSALSLPVGTLNRPRGSQSLLSPSSGYMPMNQGNLGESCQESAVSGSSERCPRPVSLHPMPRGCLASESSEGHVTGSEAELQEKVSMCRSRSRSRSPRPRGDSAYHSQRHSLLTPVTPLSPPGLEEEDVNGYVMPDTHLKGTPSSREGTLSSVGLSSVLGTEEEDEDEEYEYMNRRRRHSPPHPPRPSSLEELGYEYMDVGSDLSASLGSTQSCPLHPVPIMPTAGTTPDEDYEYMNRQRDGGGPGGDYAAMGACPASEQGYEEMRAFQGPGHQAPHVHYARLKTLRSLEATDSAFDNPDYWHSRLFPKANAQRT

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 4 - neoplasm ATC
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 4 - thyroid carcinoma DailyMed
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 4 - thyroid neoplasm EMA
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 4 Active, not recruiting thyroid cancer ClinicalTrials
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 4 - medullary thyroid gland carcinoma DailyMed
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 3 Completed non-small cell lung carcinoma ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ERBB3 PATRITUMAB Receptor tyrosine-protein kinase erbB-3 inhibitor 3 Terminated non-small cell lung carcinoma ClinicalTrials
ERBB3 POZIOTINIB Epidermal growth factor receptor inhibitor 3 Suspended non-small cell lung carcinoma ClinicalTrials
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 3 Active, not recruiting thyroid cancer ClinicalTrials
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 3 Completed thyroid cancer ClinicalTrials
ERBB3 PATRITUMAB Receptor tyrosine-protein kinase erbB-3 inhibitor 3 Terminated lung cancer ClinicalTrials
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 3 Completed lung cancer ClinicalTrials
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 3 Active, not recruiting medullary thyroid gland carcinoma ClinicalTrials
ClinicalTrials
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 3 Withdrawn medullary thyroid gland carcinoma ClinicalTrials
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 2 Completed hepatocellular carcinoma ClinicalTrials
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 2 Completed head and neck squamous cell carcinoma ClinicalTrials
ERBB3 TARLOXOTINIB Epidermal growth factor receptor inhibitor 2 Terminated head and neck squamous cell carcinoma ClinicalTrials
ERBB3 CDX-3379 Receptor tyrosine-protein kinase erbB-3 inhibitor 2 Terminated head and neck squamous cell carcinoma ClinicalTrials
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 2 Unknown status acute myeloid leukemia ClinicalTrials
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 2 Terminated clear cell renal carcinoma ClinicalTrials
ERBB3 SAPITINIB Receptor tyrosine-protein kinase erbB-3 inhibitor 2 Completed colorectal adenocarcinoma ClinicalTrials
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 2 Completed glioblastoma multiforme ClinicalTrials
ERBB3 POZIOTINIB Epidermal growth factor receptor inhibitor 2 Terminated lung adenocarcinoma ClinicalTrials
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 2 Terminated follicular thyroid carcinoma ClinicalTrials
ERBB3 VANDETANIB Epidermal growth factor receptor inhibitor 2 Terminated mesothelioma ClinicalTrials

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 intensity data of this site,
show all other sites!

ERBB3-Ser1083
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM
HNSC -0.707
LUAD
LUSC
non_ccRCC
PDAC 0.707
UCEC
ERBB3-Ser1130
Cancer Intensity
BRCA
COAD
HGSC 1.99
ccRCC -0.465
GBM 0.291
HNSC 0.168
LUAD -1.063
LUSC -0.18
non_ccRCC -0.741
PDAC
UCEC
ERBB3-Ser1315
Cancer Intensity
BRCA
COAD 0.707
HGSC -0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
ERBB3-Ser686
Cancer Intensity
BRCA -2.071
COAD 0.3
HGSC -0.053
ccRCC 0.176
GBM 0.849
HNSC 0.074
LUAD 0.314
LUSC 0.955
non_ccRCC -1.734
PDAC 0.855
UCEC 0.334
ERBB3-Ser693
Cancer Intensity
BRCA
COAD 0.707
HGSC -0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
ERBB3-Ser717
Cancer Intensity
BRCA -1.767
COAD 1.86
HGSC
ccRCC 0.331
GBM
HNSC
LUAD 0.353
LUSC -0.059
non_ccRCC -0.311
PDAC -0.176
UCEC -0.231
ERBB3-Ser982
Cancer Intensity
BRCA -1.796
COAD 0.398
HGSC 2.013
ccRCC -0.413
GBM 0.808
HNSC 0.277
LUAD -0.37
LUSC -0.474
non_ccRCC -0.906
PDAC -0.2
UCEC 0.664
ERBB3-Tyr1132
Cancer Intensity
BRCA
COAD
HGSC 0.707
ccRCC
GBM
HNSC
LUAD -0.707
LUSC
non_ccRCC
PDAC
UCEC
ERBB3-Tyr1307
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM
HNSC 0.707
LUAD -0.707
LUSC
non_ccRCC
PDAC
UCEC
ERBB3-Tyr1328
Cancer Intensity
BRCA -0.4
COAD
HGSC
ccRCC
GBM
HNSC 1.138
LUAD -0.738
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 1289 D Head and neck squamous cell carcinoma Phosphorylation 21281788
Y 1289 U Ovarian cancer Phosphorylation 20227043

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: