PAR-5359, a well-balanced PPARalpha/gamma dual agonist, exhibits equivalent antidiabetic and hypolipidemic activities in vitro and in vivo.

@article{Kim2008PAR5359AW,
  title={PAR-5359, a well-balanced PPARalpha/gamma dual agonist, exhibits equivalent antidiabetic and hypolipidemic activities in vitro and in vivo.},
  author={Mi-kyung Kim and Yu Na Chae and Moon Ho Son and Soon-Hoe Kim and Jin Kwan Kim and Ho Sang Moon and Chan Sun Park and M H Bae and Eunkyung Kim and Taedong Han and Hyun Ho Choi and Young Ah Shin and Byung-N. Ahn and Chun Ho Lee and Joong Inn Lim and Chang-Yell Shin},
  journal={European journal of pharmacology},
  year={2008},
  volume={595 1-3},
  pages={
          119-25
        }
}
Therapeutic modulators of peroxisome proliferator-activated receptors (PPAR): a patent review (2008–present)
TLDR
Recent (2008–present) patent applications concerning PPAR ligands claimed for the use in metabolic disorders as well as patents indicating new applications for modulators of the PPAR subtypes are summarized.
Dual acting and pan-PPAR activators as potential anti-diabetic therapies.
TLDR
It may be best to identify subtype-selective partial agonists or compounds that selectively activate PPAR signalling pathways and use these in combination to develop single molecules that activate two or all three PPARs.
Liquid chromatography-tandem mass spectrometry of a new PPARα/γ dual agonist PAR-5359 in rat plasma
TLDR
A reliable, selective and sensitive high-performance liquid chromatography with electrospray ionization tandem mass spectrometry was developed for the determination of PAR-5359 in rat plasma and was successfully applied to the pharmacokinetic study of PAR -5359 after oral dose at a dose of 1 mg/kg to male SD rats.
Hypolipidemic effect of hexane fraction from Rhizopus oryzae KSD-815 through peroxisome proliferator-activated receptor-α
TLDR
Results indicate that culture of R. oryzae KSD-815 may have a potent hypolipidemic activity through activation of PPAR-α and secretion of ApoA1, and in functional assay using human hepatoma HepG2 cells, RoHe-4–2 and 4–6 significantly increased apolipoprotein A1 production and showed more potent stimulation effects compared with fenofibrate.
Effect of a novel proteoglycan PTP1B inhibitor from Ganoderma lucidum on the amelioration of hyperglycaemia and dyslipidaemia in db/db mice
Protein tyrosine phosphatase 1B (PTP1B) is implicated in the negative regulation of the insulin signalling pathway by dephosphorylating the insulin receptor (IR) and IR substrates. Ganodermalucidum
Role of Apolipoprotein A1 in PPAR Signaling Pathway for Nonalcoholic Fatty Liver Disease
TLDR
The results suggested that the three PPARs might promote the expression and molecular transportation of APOA1 to form a PPAR-APOA1 signaling pathway that demonstrated a beneficial role in the pathogenesis of NAFLD.
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Results showed that pioglitazone significantly increased the apoA-I secretion from the human hepatoma cell line HepG2 and binding assay indicated that the transactivation of hPPARgamma1 or hPParalpha by piog Litazone is due to direct binding of piog litazone to each subtype.
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TLDR
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TLDR
The overall conclusions are that in db/db mice, the novel dual PPAR activator exerts potent and efficacious antidiabetic effects, preserves pancreatic insulin content, and improves metabolic abnormalities such as hyperlipidemia, fatty liver, low adiponectin levels, and elevated corticosterone levels.
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