Id: acc0176
Group: 2sens
Protein: FLT3
Gene Symbol: FLT3
Protein Id: P36888
Protein Name: FLT3_HUMAN
PTM: phosphorylation
Site: Tyr589
Site Sequence: QVTGSSDNEYFYVDFREYEYD
Disease Category: Cancer
Disease: Leukemia
Disease Subtype: AML-M5
Disease Cellline: MV4-11
Disease Info:
Drug: cabozantinib
Drug Info: "Cabozantinib is a multi-targeted tyrosine kinase inhibitor that acts on MET, VEGFR1/2/3, RET, AXL, and other kinases, approved for the treatment of progressive metastatic medullary thyroid cancer, advanced renal cell carcinoma after prior anti-angiogenic therapy, and hepatocellular carcinoma following sorafenib failure. "
Effect: modulate
Effect Info: "Cabozantinib inhibits the phosphorylation of FLT3, STAT5, AKT, and ERK, thereby inhibiting and preventing the growth of MV4 - 11 tumor cells."
Note:
Score: 4.0
Pubmed(PMID): 27060207
Sentence Index:
Sentence:

Sequence & Structure:

MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESPEDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDLQNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQDALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRECTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEMSTYSTNRTMIRILFAFVSSVARNDTGYYTCSSSKHPSQSALVTIVEKGFINATNSSEDYEIDQYEEFCFSVRFKAYPQIRCTWTFSRKSFPCEQKGLDNGYSISKFCNHKHQPGEYIFHAENDDAQFTKMFTLNIRRKPQVLAEASASQASCFSDGYPLPSWTWKKCSDKSPNCTEEITEGVWNRKANRKVFGQWVSSSTLNMSEAIKGFLVKCCAYNSLGTSCETILLNSPGPFPFIQDNISFYATIGVCLLFIVVLTLLICHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYDLKWEFPRENLEFGKVLGSGAFGKVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMSELKMMTQLGSHENIVNLLGACTLSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKEHNFSFYPTFQSHPNSSMPGSREVQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDLNVLTFEDLLCFAYQVAKGMEFLEFKSCVHRDLAARNVLVTHGKVVKICDFGLARDIMSDSNYVVRGNARLPVKWMAPESLFEGIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYKLIQNGFKMDQPFYATEEIYIIMQSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDGRVSECPHTYQNRRPFSREMDLGLLSPQAQVEDS

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
FLT3 MIDOSTAURIN Tyrosine-protein kinase receptor FLT3 inhibitor 4 - acute myeloid leukemia FDA
FLT3 GILTERITINIB FUMARATE Tyrosine-protein kinase receptor FLT3 inhibitor 4 - acute myeloid leukemia EMA
FDA
FLT3 FEDRATINIB Tyrosine-protein kinase receptor FLT3 inhibitor 4 - neoplasm ATC
FLT3 SUNITINIB Tyrosine-protein kinase receptor FLT3 inhibitor 4 Completed neoplasm ClinicalTrials
FLT3 MIDOSTAURIN Tyrosine-protein kinase receptor FLT3 inhibitor 4 - neoplasm ATC
FLT3 PEXIDARTINIB Tyrosine-protein kinase receptor FLT3 inhibitor 4 - neoplasm ATC
FLT3 PACRITINIB Tyrosine-protein kinase receptor FLT3 inhibitor 4 - neoplasm ATC
FLT3 GILTERITINIB Tyrosine-protein kinase receptor FLT3 inhibitor 4 - neoplasm ATC
FLT3 SUNITINIB Tyrosine-protein kinase receptor FLT3 inhibitor 4 - neoplasm ATC
FLT3 SUNITINIB Tyrosine-protein kinase receptor FLT3 inhibitor 4 - renal cell carcinoma DailyMed
EMA
FLT3 SORAFENIB TOSYLATE Tyrosine-protein kinase receptor FLT3 inhibitor 4 - renal cell carcinoma DailyMed
FLT3 SUNITINIB MALATE Tyrosine-protein kinase receptor FLT3 inhibitor 4 - renal cell carcinoma DailyMed
FLT3 SUNITINIB MALATE Tyrosine-protein kinase receptor FLT3 inhibitor 4 Completed renal cell carcinoma ClinicalTrials
FLT3 SUNITINIB Tyrosine-protein kinase receptor FLT3 inhibitor 4 Completed renal cell carcinoma ClinicalTrials
ClinicalTrials
FLT3 SUNITINIB Tyrosine-protein kinase receptor FLT3 inhibitor 4 Terminated renal cell carcinoma ClinicalTrials
ClinicalTrials
FLT3 PACRITINIB CITRATE Tyrosine-protein kinase receptor FLT3 inhibitor 4 - polycythemia vera FDA
FLT3 FEDRATINIB HYDROCHLORIDE Tyrosine-protein kinase receptor FLT3 inhibitor 4 - primary myelofibrosis EMA
FDA
FLT3 PACRITINIB CITRATE Tyrosine-protein kinase receptor FLT3 inhibitor 4 - primary myelofibrosis FDA
FLT3 SORAFENIB TOSYLATE Tyrosine-protein kinase receptor FLT3 inhibitor 4 - thyroid carcinoma DailyMed
FLT3 FEDRATINIB HYDROCHLORIDE Tyrosine-protein kinase receptor FLT3 inhibitor 4 - myeloproliferative disorder EMA
FLT3 MIDOSTAURIN Tyrosine-protein kinase receptor FLT3 inhibitor 4 - mast-cell leukemia DailyMed
FDA
FLT3 MIDOSTAURIN Tyrosine-protein kinase receptor FLT3 inhibitor 4 - Mastocytosis DailyMed
FLT3 PEXIDARTINIB HYDROCHLORIDE Tyrosine-protein kinase receptor FLT3 inhibitor 4 - Tenosynovial Giant Cell Tumor DailyMed
FDA
FLT3 SUNITINIB Tyrosine-protein kinase receptor FLT3 inhibitor 4 Completed pancreatic neuroendocrine tumor ClinicalTrials
FLT3 SUNITINIB MALATE Tyrosine-protein kinase receptor FLT3 inhibitor 4 - neuroendocrine neoplasm 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 842 C Acute myelogenous leukemia Phosphorylation 15345593
- - D Acute myeloid leukemia Ubiquitination 36206490
Y 842 N Acute myelogenous leukemia Phosphorylation 15345593
R 972 U Acute lymphocytic leukemia Methylation 31395602
R 972 U Acute myelogenous leukemia Methylation 31217189
R 973 U Acute lymphocytic leukemia Methylation 31395602
R 973 U Acute myelogenous leukemia Methylation 31217189
Y 591 U Acute myeloid leukemia/acute myelogenous leukemia Phosphorylation 17105820

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: