Physiological functions of peroxisome proliferator-activated receptor β
Abstract
The peroxisome proliferator-activated receptors, PPARα, PPARβ, and PPARγ, are a family of transcription factors activated by a diversity of molecules including fatty acids and fatty acid metabolites. PPARs regulate the transcription of a large variety of genes implicated in metabolism, inflammation, proliferation, and differentiation in different cell types. These transcriptional regulations involve both direct transactivation and interaction with other transcriptional regulatory pathways. The functions of PPARα and PPARγ have been extensively documented mainly because these isoforms are activated by molecules clinically used as hypolipidemic and antidiabetic compounds. The physiological functions of PPARβ remained for a while less investigated, but the finding that specific synthetic agonists exert beneficial actions in obese subjects uplifted the studies aimed to elucidate the roles of this PPAR isoform. Intensive work based on pharmacological and genetic approaches and on the use of both in vitro and in vivo models has considerably improved our knowledge on the physiological roles of PPARβ in various cell types. This review will summarize the accumulated evidence for the implication of PPARβ in the regulation of development, metabolism, and inflammation in several tissues, including skeletal muscle, heart, skin, and intestine. Some of these findings indicate that pharmacological activation of PPARβ could be envisioned as a therapeutic option for the correction of metabolic…
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PPARδ is regarded as a promising target for the treatment of metabolic syndrome because of its positive effects on serum cholesterol and lipid profiles.
“PPARd is regarded as a promising target for the treatment of metabolic syndrome because of its positive effects on serum cholesterol and lipid profiles (Neels and Grimaldi, 2014)”
From The Peroxisome Proliferator–Activated Receptor (PPAR)-γ Antagonist 2-Chloro-5-Nitro-N-Phenylbenzamide (GW9662) Triggers Perilipin 2 Expression via PPARδ and Induces Lipogenesis and Triglyceride Accumulation in Human THP-1 Macrophages (2020) · cites this paper as Neels and Grimaldi, 2014
Anti-inflammatory effects and regulatory roles in glucose metabolism have been reported for both PPARα and PPARδ.
“Furthermore, anti-inflammatory effects and regulatory roles in glucose metabolism have been reported for both isoforms (Lefebvre et al., 2006;Neels and Grimaldi, 2014;Magadum and Engel, 2018).”
From The Peroxisome Proliferator–Activated Receptor (PPAR)-γ Antagonist 2-Chloro-5-Nitro-N-Phenylbenzamide (GW9662) Triggers Perilipin 2 Expression via PPARδ and Induces Lipogenesis and Triglyceride Accumulation in Human THP-1 Macrophages (2020) · cites this paper as Neels and Grimaldi, 2014
PPARs are activated by a variety of molecules and act mainly as sensors for fatty acids and fatty acid-derived metabolites.
“PPARs are activated by a variety of molecules and act mainly as sensors for fatty acids and fatty acid-derived metabolites (Lefebvre et al., 2006;Tontonoz and Spiegelman, 2008;Neels and Grimaldi, 2014).”
From The Peroxisome Proliferator–Activated Receptor (PPAR)-γ Antagonist 2-Chloro-5-Nitro-N-Phenylbenzamide (GW9662) Triggers Perilipin 2 Expression via PPARδ and Induces Lipogenesis and Triglyceride Accumulation in Human THP-1 Macrophages (2020) · cites this paper as Neels and Grimaldi, 2014
PPARδ is ubiquitously expressed, most abundantly in tissues with high fatty acid metabolism.
“While PPARd is ubiquitously expressed (most abundantly in tissues with high fatty acid metabolism) (Neels and Grimaldi, 2014)”
From The Peroxisome Proliferator–Activated Receptor (PPAR)-γ Antagonist 2-Chloro-5-Nitro-N-Phenylbenzamide (GW9662) Triggers Perilipin 2 Expression via PPARδ and Induces Lipogenesis and Triglyceride Accumulation in Human THP-1 Macrophages (2020) · cites this paper as Neels and Grimaldi, 2014
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- Authors
- Neels, J. G., & Grimaldi, P. A.
- Affiliations
- Inserm (FR)
- ORCID
- Neels, Jaap G.
- Venue
- Physiological Reviews
- Publisher
- American Physiological Society
- Published
- 2014-07
- Volume
- 94
- Issue
- 3
- Pages
- 795-858
- ISSN
- 0031-9333 (ISSN-L)
- 1522-1210
- OpenAlex
- W2003927905
- Cited by
- 161
- References
- 60
- Citations by year
- 2026: 3 · 2025: 10 · 2024: 9 · 2023: 8 · 2022: 16 · 2021: 15 · 2020: 11 · 2019: 14 · 2018: 16 · 2017: 12 · 2016: 25 · 2015: 19 · 2014: 3
- FWCI
- 1.91
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Physiological Reviews (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Peroxisome Proliferator-Activated Receptors
- Health Sciences › Medicine › Physiology › Adipose Tissue and Metabolism
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Clinical Biochemistry › Paraoxonase enzyme and polymorphisms
- Keywords
- PPARδ, peroxisome proliferator-activated receptors, PPAR agonists, transcriptional regulation, fatty acid metabolism, inflammation, skeletal muscle, heart, skin, intestine, obesity, metabolic disorders, carcinogenesis, psoriasis
- MeSH terms
- Animals, Cell Differentiation, Humans, Inflammation, Muscles, PPAR-beta, Cell Proliferation
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