Target intelligence / Profile preview

FMS-like tyrosine kinase 3 receptor (FLT3)

Target
FLT3
Molecular classification
Receptor, Receptor Tyrosine Kinase, Class III Receptor Tyrosine Kinase
01

Overview

FMS-like tyrosine kinase 3 receptor (FLT3), also known as CD135, FLK-2, and STK-1, is a class III receptor tyrosine kinase that plays a crucial role in hematopoiesis. It is primarily expressed on immature hematopoietic progenitor cells and regulates their proliferation, survival, and differentiation. FLT3 is activated by its ligand, FLT3 ligand (FLT3L), leading to autophosphorylation and downstream signaling cascades. Mutations in FLT3, particularly internal tandem duplications (ITD) and tyrosine kinase domain mutations, are frequently found in acute myeloid leukemia (AML) and contribute to uncontrolled proliferation. FLT3 inhibitors have been developed as therapeutic agents for AML, but resistance often emerges during treatment. Dysregulation of FLT3 can also contribute to autoimmune diseases.

Other names
CD135FLK-2STK-1fetal liver kinase-2human stem cell kinase-1
02

Mechanism of action

Inhibition of FLT3 tyrosine kinase activity

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Biological functions

Cell proliferationCell survivalCell differentiationSignal transductionHematopoiesis
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Disease associations

Acute Myeloid LeukemiaAutoimmune diseasesCancer
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Safety considerations

Resistance to FLT3 inhibitorsOff-target effects of FLT3 inhibitors
06

Interacting drugs

FLT3 inhibitors
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Biomarkers

FLT3-ITD mutationsFLT3 tyrosine kinase domain mutations

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