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Target intelligence / Profile preview
Rearranged during Transfection Proto-oncogene Tyrosine-Protein Kinase (RET)
- Target
- RET
- Molecular classification
- Receptor tyrosine kinase, Proto-oncogene
01
Overview
The RET proto-oncogene encodes a receptor tyrosine kinase crucial for neural crest-derived tissue development and function. It's activated by GDNF family ligands and GFRα coreceptors. RET alterations, including gain-of-function mutations and gene fusions, are implicated in various cancers, making it an actionable therapeutic target. Selective RET inhibitors like selpercatinib and pralsetinib have shown efficacy in treating tumors with RET alterations, but resistance mechanisms can arise.
- Other names
- RET proto-oncogeneRET receptor tyrosine kinase
02
Mechanism of action
Selective RET kinase inhibitor
03
Biological functions
Signal transductionCell proliferationCell differentiationCell survivalDevelopment of enteric nervous systemKidney developmentUrinary tract developmentSpermatogenesisMetabolism
04
Disease associations
Hirschsprung’s diseaseMultiple endocrine neoplasia type 2A (MEN2A)Multiple endocrine neoplasia type 2B (MEN2B)Medullary thyroid carcinoma (MTC)PheochromocytomaPapillary thyroid carcinomaNon-small cell lung cancer (NSCLC)Cancer
05
Safety considerations
Resistance mechanisms (secondary mutations, bypass pathways)Off-target effects of inhibitors
06
Interacting drugs
Selpercatinib
1 more in the full profile.
07
Biomarkers
RET mutationsRET fusions
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