Target intelligence / Profile preview

Tyrosine-protein kinase Mer (MERTK)

Target
MERTK
Molecular classification
Receptor, Tyrosine Kinase, TYRO3/AXL/MER (TAM) receptor tyrosine kinase family
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Overview

Tyrosine-protein kinase Mer (MERTK) is a receptor tyrosine kinase that transduces signals from extracellular ligands into intracellular responses. It plays a crucial role in cell survival, migration, differentiation, and phagocytosis of apoptotic cells. MERTK is involved in immune regulation by suppressing inflammatory responses and promoting anti-inflammatory macrophage phenotypes. Mutations or dysregulation of MERTK are linked to retinitis pigmentosa and systemic autoimmune diseases. It is also being explored as a therapeutic target in cancer immunotherapy and chronic inflammatory conditions.

Other names
Proto-oncogene c-MerReceptor tyrosine kinase MerTK
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Mechanism of action

Ligand binding induces autophosphorylation at specific tyrosines, which triggers downstream signaling cascades including MAPK pathway activation.

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Biological functions

Regulation of cell survivalRegulation of cell migrationRegulation of cell differentiationPhagocytosis of apoptotic cells (efferocytosis)Modulation of cytokine productionSuppression of inflammatory responsesPlatelet aggregationCytoskeleton reorganizationInhibition or modulation of innate immune responsesPromotes anti-inflammatory M2 macrophage phenotype
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Disease associations

Autosomal recessive retinitis pigmentosaSystemic autoimmune diseaseCancerChronic inflammatory conditions
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Safety considerations

As an "innate immune checkpoint," MERTK is being explored as a therapeutic target in cancer immunotherapy and chronic inflammatory conditions; however, potential off-target effects or unintended immune modulation need careful consideration.

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