Id: acc0261
Group: 1sens
Protein: VEGFR2
Gene Symbol: KDR
Protein Id: P35968
Protein Name: VGFR2_HUMAN
PTM: phosphorylation
Site: Tyr1175
Site Sequence: ANAQQDGKDYIVLPISETLSM
Disease Category: Cancer
Disease: Hepatocellular Carcinoma
Disease Subtype:
Disease Cellline: HuH-7
Disease Info:
Drug: vandetanib
Drug Info: "Vandetanib is an oral multikinase inhibitor targeting RET, EGFR, and VEGFR, approved for the treatment of symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease."
Effect: modulate
Effect Info: "Vandetanib inhibits the phosphorylation of VEGFR - 2 and EGFR in tumor tissues, significantly reduces tumor vascular density, enhances tumor cell apoptosis, and inhibits tumor growth."
Note:
Score: 4.0
Pubmed(PMID): 22611027
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 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: