Id: acc2483
Group: 2sens
Protein: VEGFR2
Gene Symbol: KDR
Protein Id: P35968
Protein Name: VGFR2_HUMAN
PTM: phosphorylation
Site: Tyr1059
Site Sequence: ARDIYKDPDYVRKGDARLPLK
Disease Category: Cancer
Disease: Hepatocellular Carcinoma
Disease Subtype:
Disease Cellline: SMMC-7721
Disease Info:
Drug: I131-metuximab
Drug Info: "Iodine (???I) Metuximab Injection is a radioactive iodine-labeled monoclonal antibody produced by HAb18 hybridoma cells, used for the treatment of unresectable or recurrent primary hepatocellular carcinoma and advanced hepatocellular carcinoma patients who are unsuitable for or have failed transarterial chemoembolization (TACE) therapy. "
Effect: modulate
Effect Info: I131-metuximab (I131-mab) enhances its anti-cancer activity by inhibiting VEGFR-2 phosphorylation and reversing the epithelial-mesenchymal transition of hepatocellular carcinoma (HCC) cells.
Note: site unclear
Score: 4.0
Pubmed(PMID): 29210217
Sentence Index:
Sentence:

Sequence & Structure:

MQSKVLLAVALWLCVETRAASVGLPSVSLDLPRLSIQKDILTIKANTTLQITCRGQRDLDWLWPNNQSGSEQRVEVTECSDGLFCKTLTIPKVIGNDTGAYKCFYRETDLASVIYVYVQDYRSPFIASVSDQHGVVYITENKNKTVVIPCLGSISNLNVSLCARYPEKRFVPDGNRISWDSKKGFTIPSYMISYAGMVFCEAKINDESYQSIMYIVVVVGYRIYDVVLSPSHGIELSVGEKLVLNCTARTELNVGIDFNWEYPSSKHQHKKLVNRDLKTQSGSEMKKFLSTLTIDGVTRSDQGLYTCAASSGLMTKKNSTFVRVHEKPFVAFGSGMESLVEATVGERVRIPAKYLGYPPPEIKWYKNGIPLESNHTIKAGHVLTIMEVSERDTGNYTVILTNPISKEKQSHVVSLVVYVPPQIGEKSLISPVDSYQYGTTQTLTCTVYAIPPPHHIHWYWQLEEECANEPSQAVSVTNPYPCEEWRSVEDFQGGNKIEVNKNQFALIEGKNKTVSTLVIQAANVSALYKCEAVNKVGRGERVISFHVTRGPEITLQPDMQPTEQESVSLWCTADRSTFENLTWYKLGPQPLPIHVGELPTPVCKNLDTLWKLNATMFSNSTNDILIMELKNASLQDQGDYVCLAQDRKTKKRHCVVRQLTVLERVAPTITGNLENQTTSIGESIEVSCTASGNPPPQIMWFKDNETLVEDSGIVLKDGNRNLTIRRVRKEDEGLYTCQACSVLGCAKVEAFFIIEGAQEKTNLEIIILVGTAVIAMFFWLLLVIILRTVKRANGGELKTGYLSIVMDPDELPLDEHCERLPYDASKWEFPRDRLKLGKPLGRGAFGQVIEADAFGIDKTATCRTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVNLLGACTKPGGPLMVIVEFCKFGNLSTYLRSKRNEFVPYKTKGARFRQGKDYVGAIPVDLKRRLDSITSSQSSASSGFVEEKSLSDVEEEEAPEDLYKDFLTLEHLICYSFQVAKGMEFLASRKCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDARLPLKWMAPETIFDRVYTIQSDVWSFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTMLDCWHGEPSQRPTFSELVEHLGNLLQANAQQDGKDYIVLPISETLSMEEDSGLSLPTSPVSCMEEEEVCDPKFHYDNTAGISQYLQNSKRKSRPVSVKTFEDIPLEEPEVKVIPDDNQTDSGMVLASEELKTLEDRTKLSPSFGGMVPSKSRESVASEGSNQTSGYQSGYHSDDTDTTVYSSEEAELLKLIEIGVQTGSTAQILQPDSGTTLSSPPV

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
KDR CABOZANTINIB S-MALATE Vascular endothelial growth factor receptor 2 inhibitor 4 - hepatocellular carcinoma EMA
KDR MIDOSTAURIN Vascular endothelial growth factor receptor 2 inhibitor 4 - acute myeloid leukemia FDA
KDR RAMUCIRUMAB Vascular endothelial growth factor receptor 2 inhibitor 4 - neoplasm ATC
KDR LENVATINIB Vascular endothelial growth factor receptor inhibitor 4 - neoplasm ATC
KDR AXITINIB Vascular endothelial growth factor receptor inhibitor 4 - neoplasm ATC
KDR MIDOSTAURIN Vascular endothelial growth factor receptor 2 inhibitor 4 - neoplasm ATC
KDR REGORAFENIB Vascular endothelial growth factor receptor inhibitor 4 - neoplasm ATC
KDR CABOZANTINIB Vascular endothelial growth factor receptor 2 inhibitor 4 - neoplasm ATC
KDR VANDETANIB Vascular endothelial growth factor receptor inhibitor 4 - neoplasm ATC
KDR CABOZANTINIB S-MALATE Vascular endothelial growth factor receptor 2 inhibitor 4 - renal cell carcinoma EMA
DailyMed
KDR LENVATINIB MESYLATE Vascular endothelial growth factor receptor inhibitor 4 - renal cell carcinoma EMA
DailyMed
KDR TIVOZANIB HYDROCHLORIDE Vascular endothelial growth factor receptor inhibitor 4 - renal cell carcinoma FDA
DailyMed
KDR SUNITINIB Vascular endothelial growth factor receptor inhibitor 4 - neoplasm ATC
KDR SUNITINIB Vascular endothelial growth factor receptor inhibitor 4 Completed neoplasm ClinicalTrials
KDR SORAFENIB TOSYLATE Vascular endothelial growth factor receptor inhibitor 4 - renal cell carcinoma DailyMed
KDR PAZOPANIB HYDROCHLORIDE Vascular endothelial growth factor receptor inhibitor 4 - renal cell carcinoma FDA
DailyMed
KDR AXITINIB Vascular endothelial growth factor receptor inhibitor 4 - renal cell carcinoma DailyMed
DailyMed
EMA
KDR SUNITINIB MALATE Vascular endothelial growth factor receptor inhibitor 4 - renal cell carcinoma DailyMed
KDR SUNITINIB MALATE Vascular endothelial growth factor receptor inhibitor 4 Completed renal cell carcinoma ClinicalTrials
KDR PAZOPANIB HYDROCHLORIDE Vascular endothelial growth factor receptor inhibitor 4 - sarcoma FDA
DailyMed
KDR NINTEDANIB ESYLATE Vascular endothelial growth factor receptor inhibitor 4 - systemic scleroderma DailyMed
KDR SUNITINIB Vascular endothelial growth factor receptor inhibitor 4 - renal cell carcinoma DailyMed
EMA
KDR SUNITINIB Vascular endothelial growth factor receptor inhibitor 4 Completed renal cell carcinoma ClinicalTrials
ClinicalTrials
KDR SUNITINIB Vascular endothelial growth factor receptor inhibitor 4 Terminated renal cell carcinoma ClinicalTrials
ClinicalTrials
KDR NINTEDANIB ESYLATE Vascular endothelial growth factor receptor inhibitor 4 - idiopathic pulmonary fibrosis DailyMed

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
Y 951 D Head and neck squamous cell carcinoma Phosphorylation 21281788
Y 996 D Head and neck squamous cell carcinoma Phosphorylation 21281788
- - D Papillary thyroid cancer Ubiquitination 22711876
K 1041 P Prostate cancer/carcinoma/adenocarcinoma Methylation 24300896
K 1041 P Melanoma Methylation 24300896
- - U Breast cancer/tumor/carcinoma Phosphorylation 10371349
Y 1175 U Pulmonary hypertension Phosphorylation 37024132

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: