Id: acc0108
Group: 1sens
Protein: VEGFR
Gene Symbol: FLT1
Protein Id: P17948
Protein Name: VGFR1_HUMAN
PTM: phosphorylation
Site: unclear
Site Sequence:
Disease Category: Cancer
Disease: Pancreas Cancer
Disease Subtype:
Disease Cellline: L3.6pl
Disease Info:
Drug: AEE788 + gemcitabine
Drug Info: "AEE788 is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 values of 2 nM and 6 nM, respectively, and exhibits weaker activity against VEGFR2/KDR, c-Abl, c-Src, and Flt-1. Gemcitabine is a pyrimidine nucleoside analog antimetabolite and antitumor agent that inhibits DNA synthesis and repair, leading to autophagy and apoptosis. "
Effect: modulate
Effect Info: "Treatment with AEE788 alone or in combination with gemcitabine can significantly reduce the phosphorylation of EGFR and VEGFR, thereby inhibiting tumors."
Note:
Score: 4.0
Pubmed(PMID): 16026649
Sentence Index:
Sentence:

Sequence & Structure:

MVSYWDTGVLLCALLSCLLLTGSSSGSKLKDPELSLKGTQHIMQAGQTLHLQCRGEAAHKWSLPEMVSKESERLSITKSACGRNGKQFCSTLTLNTAQANHTGFYSCKYLAVPTSKKKETESAIYIFISDTGRPFVEMYSEIPEIIHMTEGRELVIPCRVTSPNITVTLKKFPLDTLIPDGKRIIWDSRKGFIISNATYKEIGLLTCEATVNGHLYKTNYLTHRQTNTIIDVQISTPRPVKLLRGHTLVLNCTATTPLNTRVQMTWSYPDEKNKRASVRRRIDQSNSHANIFYSVLTIDKMQNKDKGLYTCRVRSGPSFKSVNTSVHIYDKAFITVKHRKQQVLETVAGKRSYRLSMKVKAFPSPEVVWLKDGLPATEKSARYLTRGYSLIIKDVTEEDAGNYTILLSIKQSNVFKNLTATLIVNVKPQIYEKAVSSFPDPALYPLGSRQILTCTAYGIPQPTIKWFWHPCNHNHSEARCDFCSNNEESFILDADSNMGNRIESITQRMAIIEGKNKMASTLVVADSRISGIYICIASNKVGTVGRNISFYITDVPNGFHVNLEKMPTEGEDLKLSCTVNKFLYRDVTWILLRTVNNRTMHYSISKQKMAITKEHSITLNLTIMNVSLQDSGTYACRARNVYTGEEILQKKEITIRDQEAPYLLRNLSDHTVAISSSTTLDCHANGVPEPQITWFKNNHKIQQEPGIILGPGSSTLFIERVTEEDEGVYHCKATNQKGSVESSAYLTVQGTSDKSNLELITLTCTCVAATLFWLLLTLFIRKMKRSSSEIKTDYLSIIMDPDEVPLDEQCERLPYDASKWEFARERLKLGKSLGRGAFGKVVQASAFGIKKSPTCRTVAVKMLKEGATASEYKALMTELKILTHIGHHLNVVNLLGACTKQGGPLMVIVEYCKYGNLSNYLKSKRDLFFLNKDAALHMEPKKEKMEPGLEQGKKPRLDSVTSSESFASSGFQEDKSLSDVEEEEDSDGFYKEPITMEDLISYSFQVARGMEFLSSRKCIHRDLAARNILLSENNVVKICDFGLARDIYKNPDYVRKGDTRLPLKWMAPESIFDKIYSTKSDVWSYGVLLWEIFSLGGSPYPGVQMDEDFCSRLREGMRMRAPEYSTPEIYQIMLDCWHRDPKERPRFAELVEKLGDLLQANVQQDGKDYIPINAILTGNSGFTYSTPAFSEDFFKESISAPKFNSGSSDDVRYVNAFKFMSLERIKTFEELLPNATSMFDDYQGDSSTLLASPMLKRFTWTDSKPKASLKIDLRVTSKSKESGLSDVSRPSFCHSSCGHVSEGKRRFTYDHAELERKIACCSPPPDYNSVVLYSTPPI

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
FLT1 REGORAFENIB Vascular endothelial growth factor receptor inhibitor 4 - neoplasm ATC
FLT1 VANDETANIB Vascular endothelial growth factor receptor inhibitor 4 - neoplasm ATC
FLT1 LENVATINIB Vascular endothelial growth factor receptor inhibitor 4 - neoplasm ATC
FLT1 SUNITINIB Vascular endothelial growth factor receptor inhibitor 4 Completed neoplasm ClinicalTrials
FLT1 AXITINIB Vascular endothelial growth factor receptor inhibitor 4 - neoplasm ATC
FLT1 TIVOZANIB HYDROCHLORIDE Vascular endothelial growth factor receptor inhibitor 4 - renal cell carcinoma DailyMed
FDA
FLT1 SUNITINIB Vascular endothelial growth factor receptor inhibitor 4 - neoplasm ATC
FLT1 SUNITINIB Vascular endothelial growth factor receptor inhibitor 4 Terminated renal cell carcinoma ClinicalTrials
ClinicalTrials
FLT1 SORAFENIB TOSYLATE Vascular endothelial growth factor receptor inhibitor 4 - renal cell carcinoma DailyMed
FLT1 PAZOPANIB HYDROCHLORIDE Vascular endothelial growth factor receptor inhibitor 4 - renal cell carcinoma DailyMed
FDA
FLT1 AXITINIB Vascular endothelial growth factor receptor inhibitor 4 - renal cell carcinoma EMA
DailyMed
DailyMed
FLT1 PAZOPANIB HYDROCHLORIDE Vascular endothelial growth factor receptor inhibitor 4 - sarcoma DailyMed
FDA
FLT1 SUNITINIB MALATE Vascular endothelial growth factor receptor inhibitor 4 - renal cell carcinoma DailyMed
FLT1 SUNITINIB MALATE Vascular endothelial growth factor receptor inhibitor 4 Completed renal cell carcinoma ClinicalTrials
FLT1 LENVATINIB MESYLATE Vascular endothelial growth factor receptor inhibitor 4 - renal cell carcinoma DailyMed
EMA
FLT1 NINTEDANIB ESYLATE Vascular endothelial growth factor receptor inhibitor 4 - systemic scleroderma DailyMed
FLT1 SUNITINIB Vascular endothelial growth factor receptor inhibitor 4 - renal cell carcinoma EMA
DailyMed
FLT1 SUNITINIB Vascular endothelial growth factor receptor inhibitor 4 Completed renal cell carcinoma ClinicalTrials
ClinicalTrials
FLT1 NINTEDANIB ESYLATE Vascular endothelial growth factor receptor inhibitor 4 - idiopathic pulmonary fibrosis DailyMed
FLT1 SORAFENIB TOSYLATE Vascular endothelial growth factor receptor inhibitor 4 - thyroid carcinoma DailyMed
FLT1 LENVATINIB MESYLATE Vascular endothelial growth factor receptor inhibitor 4 - thyroid carcinoma DailyMed
FDA
FLT1 VANDETANIB Vascular endothelial growth factor receptor inhibitor 4 - thyroid carcinoma DailyMed
FLT1 VANDETANIB Vascular endothelial growth factor receptor inhibitor 4 - thyroid neoplasm EMA
FLT1 REGORAFENIB Vascular endothelial growth factor receptor inhibitor 4 - colorectal neoplasm EMA
FLT1 FRUQUINTINIB Vascular endothelial growth factor receptor inhibitor 4 - colorectal neoplasm FDA

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

No data.

PTM-Drug Perturbation Response:

source: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: