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Antidiabetic Action of a Liver X Receptor Agonist Mediated By Inhibition of Hepatic Gluconeogenesis*
TLDR
It is shown that the regulation of the liver gluconeogenic pathway by LXR agonists was a direct effect on hepatocytes, and an unanticipated role for these receptors is revealed, further linking lipid and glucose metabolism. Expand
Profiling of Zucker diabetic fatty rats in their progression to the overt diabetic state.
TLDR
At a crucial stage from 7 to 8 weeks, a reduction in insulin levels instigated several deleterious changes resulting in reduced whole-body carbohydrate utilization and increased glycemia. Expand
A tailored therapy for the metabolic syndrome: the dual peroxisome proliferator-activated receptor-alpha/gamma agonist LY465608 ameliorates insulin resistance and diabetic hyperglycemia while
TLDR
It is demonstrated that LY465608 beneficially impacts multiple facets of type 2 diabetes and associated cardiovascular risk, including those facets involved in the development of micro- and macrovascular complications, which are the major sources for morbidity and mortality in these patients. Expand
Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.
Propionic acid derivative 8, which was designed and synthesized based on putative pharmacophores of known PPARgamma- and PPARalpha-selective compounds, exhibits potent dual PPARalpha/gamma agonistExpand
Design and synthesis of a novel class of dual PPARγ/δ agonists
Abstract The design and synthesis of dual PPAR γ/δ agonist (R)-3-{2-ethyl-4-[3-(4-ethyl-2-pyridin-2-yl-phenoxy)-butoxy]-phenyl}propionic acid is described. This compound dose-dependently loweredExpand
Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
The design and synthesis of the dual peroxisome proliferator-activated receptor (PPAR) gamma/delta agonist (R)-3-{4-[3-(4-chloro-2-phenoxy-phenoxy)-butoxy]-2-ethyl-phenyl}-propionic acid (20) for theExpand
Design and synthesis of alpha-aryloxy-alpha-methylhydrocinnamic acids: a novel class of dual peroxisome proliferator-activated receptor alpha/gamma agonists.
TLDR
In preclinical models, 2 substantially improves insulin sensitivity and potently reverses diabetic hyperglycemia while significantly improving overall lipid homeostasis. Expand
Design and synthesis of dual peroxisome proliferator-activated receptors γ and δ agonists as novel euglycemic agents with a reduced weight gain profile
The design and synthesis of the dual peroxisome proliferator-activated receptor (PPAR) γ/δ agonist (R)-3-{4-[3-(4-chloro-2-phenoxy-phenoxy)-butoxy]-2-ethyl-phenyl}-propionic acid (20) for the treat...
Conversion of human-selective PPARalpha agonists to human/mouse dual agonists: a molecular modeling analysis.
TLDR
It is suggested that interaction of both 4-phenoxy and phenyloxazole substituents of these ligands with F272 and M279 in mouse PPARalpha leads to the species-specific divergence in ligand binding. Expand
Design and synthesis of novel and potent amide linked PPARγ/δ dual agonists
Abstract A series of potent amide linked PPARγ/δ dual agonists ( 1a ) has been discovered through rational design. In the ZDF rat model of type 2 diabetes, compound ( RExpand
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