Target intelligence / Profile preview

Rearranged during Transfection Proto-oncogene Tyrosine-Protein Kinase Receptor (RET)

Target
RET
Molecular classification
Receptor, Receptor Tyrosine Kinase, Proto-oncogene
01

Overview

RET encodes a receptor tyrosine kinase vital to neural development but also implicated as an oncogenic driver when mutated or aberrantly activated through gene fusion events. Its role as both a developmental regulator and cancer driver makes it an important target for genetic screening programs as well as precision oncology therapeutics using selective small-molecule inhibitors.

02

Mechanism of action

Selective RET kinase inhibitors

03

Biological functions

Signal transductionCell growthCell differentiationCell survivalNeural crest developmentKidney morphogenesis
04

Disease associations

CancerMultiple Endocrine Neoplasia type 2A/2BPapillary Thyroid CarcinomaNon-Small Cell Lung CancerHirschsprung’s Disease
05

Safety considerations

Resistance to RET inhibitors due to secondary mutationsOff-target effects of RET inhibitors
06

Interacting drugs

Selpercatinib

1 more in the full profile.

07

Biomarkers

RET mutations (e.g., M918T)RET fusions (e.g., KIF5B-RET, CCDC6-RET)

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