Id: acc0100
Group: 1sens
Protein: VEGFR2
Gene Symbol: KDR
Protein Id: P35968
Protein Name: VGFR2_HUMAN
PTM: phosphorylation
Site: Tyr1054
Site Sequence: CDFGLARDIYKDPDYVRKGDA
Disease Category: Cancer
Disease: Skin Cancer
Disease Subtype: SCC
Disease Cellline: Colo16
Disease Info:
Drug: AEE788
Drug Info: "AEE788 is a potent inhibitor of EGFR (IC50 = 2 nM) and HER2/ErbB2 (IC50 = 6 nM) with weaker activity against VEGFR2/KDR, c-Abl, c-Src, and Flt-1 (IC50 = 50-80 nM), while showing no inhibition against Ins-R, IGF-1R, PKCalpha, or CDK1."
Effect: modulate
Effect Info: "AEE788 inhibits the phosphorylation of EGFR, VEGFR - 2, Akt, and MAPK, thereby inhibiting tumors."
Note:
Score: 4.0
Pubmed(PMID): 15756022
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: