Target intelligence / Profile preview

MER tyrosine kinase receptor (MERTK)

Target
MERTK
Molecular classification
Receptor tyrosine kinase, TAM receptor kinase family
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Overview

MER tyrosine kinase receptor (MERTK) is a member of the TAM (TYRO3, AXL, MER) receptor tyrosine kinase family. It plays a crucial role in efferocytosis, the process of engulfing apoptotic cells, thereby maintaining tissue homeostasis and preventing autoimmunity. MERTK is expressed on various cells of the innate immune system and modulates cytokine production, limiting inflammatory responses. Aberrant expression or mutations in MERTK are implicated in diseases such as retinitis pigmentosa and cancer, making it a therapeutic target for these conditions. Targeting Mer may improve event-free survival rates while reducing therapy toxicity in ALL patients; similar strategies may be applicable across other cancers where Mer is overexpressed or dysregulated. Loss or dysfunction leads to impaired efferocytosis, increased unengulfed apoptotic bodies, altered macrophage populations/polarization states, iron accumulation due to defective hemoglobin turnover—implicating MerTK as a therapeutic target for fibrotic/immune-mediated diseases.

Other names
c-mer proto-oncogene tyrosine kinase
02

Mechanism of action

Inhibition of MERTK kinase activity, reducing pro-survival signaling pathways such as AKT and MAPK.

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Biological functions

EfferocytosisPhagocytosisImmune modulationImmune suppressionCell survival
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Disease associations

Retinitis pigmentosaCancerFibrosisInflammationAutoimmune disease
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Safety considerations

Potential for off-target effects due to kinase inhibitor promiscuity.Potential for immune dysregulation due to disruption of MERTK-mediated immune homeostasis.

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