Target intelligence / Profile preview

Mer receptor tyrosine kinase (MerTK)

Target
MerTK
Molecular classification
Receptor tyrosine kinase, TAM family receptor
01

Overview

MerTK is a receptor tyrosine kinase belonging to the TAM family. It plays a crucial role in efferocytosis, platelet function, and immune regulation. As an innate immune checkpoint, it is often exploited by cancer cells to suppress anti-tumor immunity, making it a target for cancer immunotherapy. Ligands include GAS6 and PROS1, which induce receptor dimerization and autophosphorylation, activating downstream signaling pathways like MAPK/ERK and PI3K/AKT.

Other names
c-mer proto-oncogene tyrosine kinaseProto-oncogene tyrosine-protein kinase MER
02

Mechanism of action

Inhibition of MerTK kinase activity, blocking downstream signaling pathways

03

Biological functions

EfferocytosisPlatelet functionCytoskeleton reorganizationImmune regulationPhagocytosis
04

Disease associations

Retinitis pigmentosaCancerAutoimmune diseasesInflammatory diseases
05

Safety considerations

Potential for off-target effects due to kinase similarityImmune-related adverse eventsThrombocytopenia
06

Biomarkers

MERTK expression level in tumor tissueGAS6 levels

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