PPARs as Nuclear Receptors for Nutrient and Energy Metabolism

Hong, Fan; Pan, Shijia; Yuan, Guo; Xu, Pengfei; Zhai, Yonggong

doi:10.3390/molecules24142545

Cited by 156 publications

(117 citation statements)

References 166 publications

(200 reference statements)

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“…Since their identification as receptors responsible for peroxisome proliferation in 1990, research on peroxisome proliferator‐activated receptors (PPARs) has increased dramatically, revealing more and more fascinating functions in human biology. This research also has revealed that dysregulation of PPARs is connected to the development of a wide range of human diseases, including atherosclerosis, obesity, type 2 diabetes and many others …”

Section: Ppars In Human Biology and Skinmentioning

confidence: 99%

“…PPARs are nuclear hormone receptors abundantly expressed in tissues that display high fatty acid metabolism, including human skin and its appendages . Three different isoforms of PPARs exist—PPAR‐α, PPAR‐β/δ and PPAR‐γ, which demonstrate diverse functional capabilities, including—to name but a few examples—the control of lipogenesis, cell cycle and inflammatory gene expression (Figure ) …”

Section: Ppars In Human Biology and Skinmentioning

confidence: 99%

“…control of lipogenesis, cell cycle and inflammatory gene expression ( Figure 1). [4,5,39,40] PPARs are transcription factors that regulate gene transcription either negatively or positively. They are activated by binding of specific ligands or by kinase-mediated phosphorylation.…”

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confidence: 99%

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PPAR‐γ signalling as a key mediator of human hair follicle physiology and pathology

Ramot

Bertolini

Boboljova

et al. 2019

Experimental Dermatology

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Peroxisome proliferator‐activated receptors (PPARs) are abundantly expressed in human skin, with PPAR‐γ being the most intensively investigated isoform. In various ex vivo and in vivo models, PPAR‐γ‐mediated signalling has recently surfaced as an essential element of hair follicle (HF) development, growth and stem cell biology. Moreover, the availability of novel, topically applicable PPAR‐γ modulators with a favourable toxicological profile has extended the range of potential applications in clinical dermatology. In this review, we synthesize where this field currently stands and sketch promising future research avenues, focussing on the role of PPAR‐γ‐mediated signalling in the biology and pathology of human scalp HFs, with special emphasis on scarring alopecias such as lichen planopilaris and frontal fibrosing alopecia as model human epithelial stem cell diseases. In particular, we discuss whether and how pharmacological modulation of PPAR‐γ signalling may be employed for the management of hair growth disorders, for example, in scarring alopecia (by reducing HF inflammation as well as by promoting the survival and suppressing pathological epithelial‐mesenchymal transition of keratin 15 + epithelial stem cells in the bulge) and in hirsutism/hypertrichosis (by promoting catagen development). Moreover, we explore the potential role of PPAR‐γ in androgenetic alopecia, HF energy metabolism and HF ageing, and consider clinical perspectives that emanate from the limited data available on this so far. As this field of translational human hair research is still in its infancy, many open questions exist, for which we briefly delineate selected experimental approaches that promise to generate instructive answers in the near future.

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Section: Ppars In Human Biology and Skinmentioning

confidence: 99%

Section: Ppars In Human Biology and Skinmentioning

confidence: 99%

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PPAR‐γ signalling as a key mediator of human hair follicle physiology and pathology

Ramot

Bertolini

Boboljova

et al. 2019

Experimental Dermatology

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“…Additionally, compounds 1 and 2 were evaluated for agonist activity to peroxisome proliferator-activated receptors (PPARs) because similar oxo fatty acids are known to act as PPAR agonists [42]. PPARs are ligand-activated transcription factors playing key roles in lipid and carbohydrate metabolism [43,44]. PPARα upregulates lipid uptake and β-oxidation of fatty acids, whereas PPARγ promotes adipocyte differentiation and adipokine production in adipose tissues to improve insulin sensitivity in diabetic patients [45][46][47].…”

Section: Resultsmentioning

confidence: 99%

Two antibacterial and PPARα/γ-agonistic unsaturated keto fatty acids from a coral-associated actinomycete of the genus Micrococcus

Sharma¹,

Harunari²,

Oku³

et al. 2020

Beilstein J. Org. Chem.

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A pair of geometrically isomeric unsaturated keto fatty acids, (6E,8Z)- and (6E,8E)-5-oxo-6,8-tetradecadienoic acids (1 and 2), were isolated from the culture broth of an actinomycete of the genus Micrococcus, which was associated with a stony coral, Catalaphyllia sp. Their chemical structures were elucidated by spectroscopic analysis including NMR and MS, with special assistance of spin system simulation studies for the assignment of an E geometry at C8 in 2. As metabolites of microbes, compounds 1 and 2 are unprecedented in terms of bearing a 2,4-dienone system. Both 1 and 2 showed antibacterial activity against the plant pathogen Rhizobium radiobacter and the fish pathogen Tenacibaculum maritimum, with a contrasting preference that 1 is more effective to the former strain while 2 is so to the latter. In addition, compounds 1 and 2 displayed agonistic activity against peroxisome proliferator-activated receptors (PPARs) with an isoform specificity towards PPARα and PPARγ.

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“…The peroxisome proliferator‐activated receptor δ (PPARδ) is a nuclear receptor and belongs to the PPAR family, which includes PPARα, PPARγ and PPARδ. [ 13–15 ] The agonist of PPARα (fenofibrate) or PPARγ (rosiglitazone) has been widely used to the treatment of dyslipidemia and T2DM, but the adverse effects limited its application. [ 16–18 ] PPARδ, another member of the PPAR family, exhibits high expression levels not only in liver but also in skeletal muscle and macrophages, and its activation ameliorates anti‐inflammation, insulin sensitization and lipid metabolism.…”

Section: Introductionmentioning

confidence: 99%

HWL-088, a new and highly effective FFA1/PPARδ dual agonist, attenuates nonalcoholic steatohepatitis by regulating lipid metabolism, inflammation and fibrosis

Zhou

Deng

et al. 2020

Journal of Pharmacy and Pharmacology

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Objectives Nonalcoholic fatty liver (NAFLD), a chronic progressive liver disease, is highly correlated with pathoglycemia, dyslipidemia and oxidative stress. The free fatty acid receptor 1 (FFA1) agonists have been reported to improve liver steatosis and fibrosis, and the peroxisome proliferator-activated receptor d (PPARd) plays a synergistic role with FFA1 in energy metabolism and fibrosis. HWL-088, a PPARd/FFA1 dual agonist, exerts better glucose-lowering effects than the representative FFA1 agonist TAK-875. However, the ability of HWL-088 to protect NAFLD was unknown. This study aimed to discover a new strategy for the treatment of NAFLD. Methods The methionine-and choline-deficient diet (MCD)-induced Nonalcoholic steatohepatitis (NASH) model was constructed to evaluate the effects of HWL-088. Key findings Administration of HWL-088 exerted multiple benefits on glucose control, lipid metabolism and fatty liver. Further mechanism research indicated that HWL-088 promotes lipid metabolism by decreasing lipogenesis and increasing lipolysis. Moreover, HWL-088 attenuates NASH by regulating the expression levels of genes related to inflammation, fibrosis and oxidative stress. Conclusions These positive results indicated that PPARd/FFA1 dual agonist HWL-088 might be a potential candidate to improve multiple pathogenesis of NASH.

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PPARs as Nuclear Receptors for Nutrient and Energy Metabolism

Cited by 156 publications

References 166 publications

PPAR‐γ signalling as a key mediator of human hair follicle physiology and pathology

PPAR‐γ signalling as a key mediator of human hair follicle physiology and pathology

Two antibacterial and PPARα/γ-agonistic unsaturated keto fatty acids from a coral-associated actinomycete of the genus Micrococcus

HWL-088, a new and highly effective FFA1/PPARδ dual agonist, attenuates nonalcoholic steatohepatitis by regulating lipid metabolism, inflammation and fibrosis

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