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Receptor-mediated activation of ceramidase activity initiates the pleiotropic actions of adiponectin
TLDR
Observations suggest a unifying mechanism of action for the beneficial systemic effects exerted by adiponectin, with sphingolipid metabolism as its core upstream signaling component.
Development of a supersaturable SEDDS (S-SEDDS) formulation of paclitaxel with improved oral bioavailability.
TLDR
In vitro dilution of the S-SEDDS formulation results in formation of a microemulsion, followed by slow crystallization of paclitaxel on standing, indicating that the system is supersaturated with respect to crystalline pac litaxel, and the supersaturated state is prolonged by HPMC in the formulation.
Pharmacological Inhibition of Nicotinamide Phosphoribosyltransferase (NAMPT), an Enzyme Essential for NAD+ Biosynthesis, in Human Cancer Cells
TLDR
The effects of FK866, a small molecule inhibitor of NAMPT currently in clinical trials, on glycolysis, the pentose phosphate pathway, the tricarboxylic acid (TCA) cycle, and serine biosynthesis in cancer cells and tumor xenografts are examined.
AGPAT6 Is a Novel Microsomal Glycerol-3-phosphate Acyltransferase*
TLDR
It is shown that AGPAT6 is a microsomal glycerol-3-phosphate acyltransferase (GPAT), and a renaming of this enzyme GPAT4 is proposed.
M1 and M2 Muscarinic Receptor Subtypes Regulate Antidepressant-Like Effects of the Rapidly Acting Antidepressant Scopolamine
TLDR
Muscarinic M1 and M2 receptors are established as sufficient to generate behavioral effects consistent with an antidepressant phenotype and therefore as potential targets in the antidepressant effects of scopolamine.
Impaired de Novo Choline Synthesis Explains Why Phosphatidylethanolamine N-Methyltransferase-deficient Mice Are Protected from Diet-induced Obesity*
TLDR
De novo synthesis of choline via PEMT has a previously unappreciated role in regulating whole body energy metabolism and is linked to diet-induced obesity.
Reducing Plasma Membrane Sphingomyelin Increases Insulin Sensitivity
TLDR
It is concluded that Sptlc2 heterozygous deficiency- or Sms2 deficiency-mediated reduction of SM in the plasma membranes leads to an improvement in tissue and whole-body insulin sensitivity.
Sphingomyelin Synthase 2 Deficiency Attenuates NF&kgr;B Activation
TLDR
SMS2 is a modulator ofNF&kgr;B activation, and thus it could play an important role in NF&k gr;B-mediated proatherogenic process.
A panel of cytochrome P450 BM3 variants to produce drug metabolites and diversify lead compounds.
Herein we demonstrate that a small panel of variants of cytochrome P450 BM3 from Bacillus megaterium covers the breadth of reactivity of human P450s by producing 12 of 13 mammalian metabolites for
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