Christian Guenat

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Careful regulation of mRNA half-lives is a fundamental mechanism allowing cells to quickly respond to changing environmental conditions. The mRNA-binding Hu proteins are important for stabilization of short-lived mRNAs. Here we describe the identification and mechanistic characterization of the first low-molecular-weight inhibitors for Hu protein R (HuR)(More)
The high mass accuracy and resolution of Fourier transform (FT)-ion cyclotron resonance (ICR) mass spectrometry are making it an increasingly useful tool in drug discovery and development. The basics of FT-ICR are described here, including modern ion sources and fragmentation methods. Although FT-ICR is not a high-throughput method in the traditional sense,(More)
In this article, the authors discuss 9-hydroxymethyl-10-carbamoyl acridan (9-OH-CBZ), another metabolite of carbamazepine (CBZ) found in serum. The retention time of unconjugated 9-OH-CBZ should be known when using a chromatographic method, because it appears in concentrations varying from one eighth to one third of the CBZ-10,11-epoxide (CBZ-E)(More)
Synthetic modification of cyclosporin A at P3-P4 positions led to the discovery of NIM258, a next generation cyclophilin inhibitor with excellent anti-hepatitis C virus potency, with decreased transporter inhibition, and pharmacokinetics suitable for coadministration with other drugs. Herein is disclosed the evolution of the synthetic strategy to from the(More)
We have proposed, using styrene as a model, a new mechanism for the formation of glutathione conjugates that is independent of epoxide formation but dependent on the oxidation of glutathione to a thiyl radical by peroxidases such as prostaglandin H synthase or horseradish peroxidase. The thiyl radical reacts with styrene to yield a carbon-centered radical(More)
INTRODUCTION There is limited information on in vitro/ex vivo tools to be used for studying interorgan metabolic cooperation. We report here the use of the tissue slice technique for this purpose. METHODS Rat liver and kidney slices were used to study metabolic cooperation for the metabolism of CGP 47 969, a potential anti-inflammatory compound which in(More)
A stable nonreducible trifunctional cross-linking amino acid has been isolated from mature bovine skin collagen fibrils. Previous cross-link peptide isolations and amino acid analyses indicate the compound has properties identical with those of hydroxyaldolhistidine. Its newly proposed structure was verified using fast atom bombardment mass spectrometry,(More)
The effects of 3-methylcholanthrene and phénobarbitaltreatment on the adult rat hepatic cytosolic glucocorticoid (GRc) receptor were inves tigated. Analyses of sucrose gradient profiles and equilibrium binding data of ('H]dexamet nasone bound to the GRc revealed that administration of 3-methylcholanthrene (20-40 mg/kg daily i.p. for 2 days) to adult female(More)
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