Target intelligence / Profile preview

Proto-oncogene Tyrosine-Protein Kinase RET (RET)

Target
RET
Molecular classification
Receptor tyrosine kinase, Receptor
01

Overview

The RET protein is a receptor tyrosine kinase that plays a crucial role in cell signaling pathways regulating cell proliferation, migration, differentiation, survival, and maturation. It is essential for the normal development of the enteric nervous system, autonomic nervous system, and kidneys. RET acts as a cell-surface receptor for glial cell line-derived neurotrophic factor (GDNF) family ligands via GFRα coreceptors. Mutations in RET can lead to developmental disorders like Hirschsprung's disease (loss-of-function) or various cancers such as multiple endocrine neoplasia and papillary thyroid carcinoma (gain-of-function).

Other names
Rearranged during Transfection
02

Mechanism of action

RET kinase inhibition

03

Biological functions

Signal transductionCell proliferationCell migrationCell differentiationCell survivalCell maturationDevelopment of enteric nervous systemDevelopment of autonomic nervous systemKidney developmentSpermatogenesisBody weight regulation
04

Disease associations

Hirschsprung’s diseaseMultiple endocrine neoplasia type II A/BPapillary thyroid carcinomaPheochromocytomaParathyroid hyperplasiaNon-small cell lung cancerCancer
05

Safety considerations

On-target toxicities due to inhibition of RET signaling in normal tissuesResistance development
06

Biomarkers

RET mutations in tumorsRET fusion transcripts

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