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PPAR Agonists and Metabolic Syndrome: An Established Role?

International journal of molecular sciences, 2018-04, Vol.19 (4), p.1197 [Peer Reviewed Journal]

2018 by the authors. 2018 ;ISSN: 1422-0067 ;EISSN: 1422-0067 ;DOI: 10.3390/ijms19041197 ;PMID: 29662003

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Title:
PPAR Agonists and Metabolic Syndrome: An Established Role?
Author: Botta, Margherita ; Audano, Matteo ; Sahebkar, Amirhossein ; Sirtori, Cesare R ; Mitro, Nico ; Ruscica, Massimiliano
Subjects: Animals ; Benzoxazoles - chemistry ; Benzoxazoles - pharmacology ; Benzoxazoles - therapeutic use ; Butyrates - chemistry ; Butyrates - pharmacology ; Butyrates - therapeutic use ; Chalcones - chemistry ; Chalcones - pharmacology ; Chalcones - therapeutic use ; Drug Discovery ; elafibrinor ; Humans ; Hypoglycemic Agents - chemistry ; Hypoglycemic Agents - pharmacology ; Hypoglycemic Agents - therapeutic use ; Hypolipidemic Agents - chemistry ; Hypolipidemic Agents - pharmacology ; Hypolipidemic Agents - therapeutic use ; Insulin Resistance ; Lipid Metabolism - drug effects ; Lipids - blood ; metabolic syndrome ; Metabolic Syndrome - blood ; Metabolic Syndrome - drug therapy ; Metabolic Syndrome - metabolism ; pemafibrate ; Peroxisome Proliferator-Activated Receptors - agonists ; Peroxisome Proliferator-Activated Receptors - metabolism ; PPARs ; Propionates - chemistry ; Propionates - pharmacology ; Propionates - therapeutic use ; Review ; Thiazolidinediones - chemistry ; Thiazolidinediones - pharmacology ; Thiazolidinediones - therapeutic use ; Triglycerides - blood ; Triglycerides - metabolism
Is Part Of: International journal of molecular sciences, 2018-04, Vol.19 (4), p.1197
Description: Therapeutic approaches to metabolic syndrome (MetS) are numerous and may target lipoproteins, blood pressure or anthropometric indices. Peroxisome proliferator-activated receptors (PPARs) are involved in the metabolic regulation of lipid and lipoprotein levels, i.e., triglycerides (TGs), blood glucose, and abdominal adiposity. PPARs may be classified into the α, β/δ and γ subtypes. The PPAR-α agonists, mainly fibrates (including newer molecules such as pemafibrate) and omega-3 fatty acids, are powerful TG-lowering agents. They mainly affect TG catabolism and, particularly with fibrates, raise the levels of high-density lipoprotein cholesterol (HDL-C). PPAR-γ agonists, mainly glitazones, show a smaller activity on TGs but are powerful glucose-lowering agents. Newer PPAR-α/δ agonists, e.g., elafibranor, have been designed to achieve single drugs with TG-lowering and HDL-C-raising effects, in addition to the insulin-sensitizing and antihyperglycemic effects of glitazones. They also hold promise for the treatment of non-alcoholic fatty liver disease (NAFLD) which is closely associated with the MetS. The PPAR system thus offers an important hope in the management of atherogenic dyslipidemias, although concerns regarding potential adverse events such as the rise of plasma creatinine, gallstone formation, drug-drug interactions (i.e., gemfibrozil) and myopathy should also be acknowledged.
Publisher: Switzerland: MDPI
Language: English
Identifier: ISSN: 1422-0067
EISSN: 1422-0067
DOI: 10.3390/ijms19041197
PMID: 29662003
Source: MEDLINE
PubMed Central
ProQuest Central
DOAJ Directory of Open Access Journals

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PPAR Agonists and Metabolic Syndrome: An Established Role?

2018 by the authors. 2018 ;ISSN: 1422-0067 ;EISSN: 1422-0067 ;DOI: 10.3390/ijms19041197 ;PMID: 29662003

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