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Target intelligence / Profile preview
Peroxisome Proliferator-Activated Receptors (PPARs)
- Target
- PPARs
- Molecular classification
- Nuclear hormone receptor, Transcription factor, NR1C subfamily
01
Overview
Peroxisome proliferator-activated receptors (PPARs) are a group of nuclear hormone receptors that function as ligand-activated transcription factors. They regulate lipid metabolism, glucose homeostasis, cellular differentiation, proliferation, and inflammation. The PPAR family consists of three main isotypes: PPAR-alpha, PPAR-delta/beta, and PPAR-gamma. They form heterodimers with RXR and bind to PPREs to modulate gene expression. Dysregulation is implicated in metabolic syndrome, type 2 diabetes, atherosclerosis, and cancer.
- Other names
- NR1C1PPAR-alphaPPARαNR1C2PPAR-deltaPPARδPPAR-betaPPARβNR1C3PPAR-gammaPPARγ
02
Mechanism of action
PPARs form heterodimers with RXR, bind to PPREs on target gene promoters, and modulate transcription by recruiting coactivators or corepressors.
03
Biological functions
Lipid metabolismGlucose homeostasisCellular differentiationCell proliferationInflammationAdipogenesisFatty acid oxidationWound healingLipid uptakeLipid storage
04
Disease associations
Metabolic syndromeType 2 diabetes mellitusAtherosclerosisCancer (progression/inhibition)
05
Safety considerations
Dysregulated PPAR activity implicated in various diseasesContext-dependent effects in cancer (progression or inhibition)
06
Interacting drugs
Fibrate drugs
2 more in the full profile.
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