Target intelligence / Profile preview

Tyrosine-protein kinase receptor FLT3 (FLT3)

Target
FLT3
Molecular classification
Receptor, Tyrosine Kinase, Receptor Tyrosine Kinase (RTK), Class III receptor tyrosine kinase
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Overview

Tyrosine-protein kinase receptor FLT3 (FLT3) is a receptor tyrosine kinase that plays a crucial role in hematopoiesis, regulating the differentiation, proliferation, and survival of hematopoietic progenitor cells. Mutations in FLT3, particularly internal tandem duplications (FLT3-ITD) and point mutations at D835, are common in acute myeloid leukemia (AML) and drive uncontrolled proliferation and resistance to apoptosis. FLT3 is a therapeutic target, and FLT3 inhibitors have been developed for AML treatment.

Other names
Fms-like tyrosine kinase 3Stem cell tyrosine kinase 1Fetal liver kinase-2CD135
02

Mechanism of action

Inhibition of FLT3 kinase activity, either by binding to the ATP-binding site (Type I) or preventing activation by occupying a hydrophobic region (Type II).

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Biological functions

Signal transductionCell proliferationCell differentiationCell survivalHematopoiesisGrowth factor signalingKinase activity
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Disease associations

Acute myeloid leukemia (AML)Cancer
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Safety considerations

Resistance to FLT3 inhibitorsOff-target effects of kinase inhibitors
06

Interacting drugs

FLT3 inhibitors (Type I and Type II)
07

Biomarkers

FLT3-ITD mutationsFLT3 D835 mutations

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