Id: | acc3238 |
Group: | 2sens |
Protein: | VEGFR2 |
Gene Symbol: | KDR |
Protein Id: | P35968 |
Protein Name: | VGFR2_HUMAN |
PTM: | phosphorylation |
Site: | Tyr1175 |
Site Sequence: | ANAQQDGKDYIVLPISETLSM |
Disease Category: | Cardiovascular and circulatory system diseases |
Disease: | Angiogenesis |
Disease Subtype: | |
Disease Cellline: | HUVEC |
Disease Info: | |
Drug: | Triphala churna |
Drug Info: | "Triphala churna is an Ayurvedic herbal formulation known for its health - promoting properties, often used to support digestion." |
Effect: | modulate |
Effect Info: | "THL significantly and specifically inhibits VEGF-induced angiogenesis by suppressing the phosphorylation of (VEGFR-2), thereby inhibiting tumors." |
Note: | |
Score: | 4.0 |
Pubmed(PMID): | 22937129 |
Sentence Index: | 22937129_4-5 |
Sentence: | "Because vascular endothelial growth factor-A (VEGF) induced angiogenesis plays a critical role in the pathogenesis of cancer, we therefore investigated whether tumor inhibitory effects of THL or its active constituents are through suppression of VEGF actions. We herein report that THL and chebulinic (CI) present in THL can significantly and specifically inhibit VEGF induced angiogenesis by suppressing VEGF receptor-2 (VEGFR-2) phosphorylation." |
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.