Target intelligence / Profile preview

Receptor tyrosine-protein kinase RET (RET)

Target
RET
Molecular classification
Receptor, Receptor Tyrosine Kinase
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Overview

RET (Rearranged during Transfection) is a receptor tyrosine kinase that plays essential roles in cell signaling, particularly in the development and maintenance of neural crest-derived cells, the urogenital system, and both central and peripheral nervous systems. It is crucial for kidney development, enteric neuron formation, and spermatogenesis. Mutations in RET are associated with various diseases, including Hirschsprung's disease and several types of cancer. Activation occurs through ligand binding to GFRα co-receptors, leading to RET dimerization and autophosphorylation.

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Mechanism of action

Tyrosine kinase inhibition

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Biological functions

Signal transductionCell survivalCell proliferationCell differentiationNeuronal developmentKidney morphogenesisSpermatogenesis
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Disease associations

CancerHirschsprung's diseaseMultiple endocrine neoplasia type 2A/2BPapillary thyroid carcinomaPheochromocytomaParathyroid hyperplasia
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Safety considerations

Off-target effects of RET inhibitorsDevelopmental toxicity
06

Biomarkers

RET mutations (e.g., in thyroid cancer)RET fusions

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