Id: | acc0509 |
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: | Bladder Cancer |
Disease Subtype: | |
Disease Cellline: | T24 |
Disease Info: | |
Drug: | AE-AS |
Drug Info: | - |
Effect: | modulate |
Effect Info: | AE-AS can significantly reduce the phosphorylation of VEGFR2 and simultaneously reduce tumor growth. |
Note: | |
Score: | 4.0 |
Pubmed(PMID): | 28710377 |
Sentence Index: | 28710377_5 |
Sentence: | "Treatment with AE-AS markedly decreased the protein accumulation and transcriptional activity of HIF-1alpha, vascular endothelial growth factor (VEGF) expression/secretion, and VEGFR2 phosphorylation in hypoxic human bladder cancer (T24) cells and tumor tissues accompanied by a reduction of tumor growth." |
Sequence & Structure:
MQSKVLLAVALWLCVETRAASVGLPSVSLDLPRLSIQKDILTIKANTTLQITCRGQRDLDWLWPNNQSGSEQRVEVTECSDGLFCKTLTIPKVIGNDTGAYKCFYRETDLASVIYVYVQDYRSPFIASVSDQHGVVYITENKNKTVVIPCLGSISNLNVSLCARYPEKRFVPDGNRISWDSKKGFTIPSYMISYAGMVFCEAKINDESYQSIMYIVVVVGYRIYDVVLSPSHGIELSVGEKLVLNCTARTELNVGIDFNWEYPSSKHQHKKLVNRDLKTQSGSEMKKFLSTLTIDGVTRSDQGLYTCAASSGLMTKKNSTFVRVHEKPFVAFGSGMESLVEATVGERVRIPAKYLGYPPPEIKWYKNGIPLESNHTIKAGHVLTIMEVSERDTGNYTVILTNPISKEKQSHVVSLVVYVPPQIGEKSLISPVDSYQYGTTQTLTCTVYAIPPPHHIHWYWQLEEECANEPSQAVSVTNPYPCEEWRSVEDFQGGNKIEVNKNQFALIEGKNKTVSTLVIQAANVSALYKCEAVNKVGRGERVISFHVTRGPEITLQPDMQPTEQESVSLWCTADRSTFENLTWYKLGPQPLPIHVGELPTPVCKNLDTLWKLNATMFSNSTNDILIMELKNASLQDQGDYVCLAQDRKTKKRHCVVRQLTVLERVAPTITGNLENQTTSIGESIEVSCTASGNPPPQIMWFKDNETLVEDSGIVLKDGNRNLTIRRVRKEDEGLYTCQACSVLGCAKVEAFFIIEGAQEKTNLEIIILVGTAVIAMFFWLLLVIILRTVKRANGGELKTGYLSIVMDPDELPLDEHCERLPYDASKWEFPRDRLKLGKPLGRGAFGQVIEADAFGIDKTATCRTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVNLLGACTKPGGPLMVIVEFCKFGNLSTYLRSKRNEFVPYKTKGARFRQGKDYVGAIPVDLKRRLDSITSSQSSASSGFVEEKSLSDVEEEEAPEDLYKDFLTLEHLICYSFQVAKGMEFLASRKCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDARLPLKWMAPETIFDRVYTIQSDVWSFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTMLDCWHGEPSQRPTFSELVEHLGNLLQANAQQDGKDYIVLPISETLSMEEDSGLSLPTSPVSCMEEEEVCDPKFHYDNTAGISQYLQNSKRKSRPVSVKTFEDIPLEEPEVKVIPDDNQTDSGMVLASEELKTLEDRTKLSPSFGGMVPSKSRESVASEGSNQTSGYQSGYHSDDTDTTVYSSEEAELLKLIEIGVQTGSTAQILQPDSGTTLSSPPV
Select PDB:
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 TargetsPTM Intensity:
source: CPTACNo data.
PTM-Disease Association:
source: PTMDResidue | 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: DecryptMNo data.
Function score:
source: funscoRNo data.