Publications by authors named "M Adenot"

A retrospective analysis was conducted in a French pediatric hospital in Lyon. Subjects were 16 patients diagnosed with acute viral encephalitis with identified causative agents who were admitted to the pediatric intensive care unit from 2008 to 2011. The median length of stay was 6 days.

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Background: SynB family peptides conjugated to several drugs have been shown to increase the brain uptake and in vivo activities of these drugs via an adsorptive-mediated transcytosis mechanism. Based on both in vivo and in vitro experimental data, a cell uptake component has been added to our computational model of blood-brain barrier.

Methods: In situ brain perfusion, in vitro cell model and a computational cell uptake model have been used to discover brain-penetrating properties of SynB peptides and to screen libraries of new rationally designed peptide vectors suitable for brain drug delivery.

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Except for a few well-documented CNS therapeutics, quantitative data on blood-brain barrier (BBB) permeation is incomplete, unreliable or nonexistent and this is a major impediment in BBB modeling. Furthermore, only the passive diffusion component is generally taken into account. Three techniques of modeling (in vivo, in vitro and in silico) were set up and compared.

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Glucagon-like peptide-1 (GLP-1) is a 30-residue peptide implicated in short-term appetite regulation. Its analogs are presumed to be potential drugs against obesity and non-insulin dependent diabetes mellitus (NIDDM or type 2 diabetes). This study examined how the dynamic fingerprints can be used for establishing dynamics-activity relationships in a series of peptides for which the mechanism of action is unknown and in which mutations can cause an increase or decrease in biological activity.

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The aim of this article is to present the design of a large heterogeneous CNS library (approximately 1700 compounds) from WDI and mapping CNS drugs using QSAR models of blood-brain barrier (BBB) permeation and P-gp substrates. The CNS library finally includes 1336 BBB-crossing drugs (BBB+), 259 molecules non-BBB-crossing (BBB-), and 91 P-gp substrates (either BBB+ or BBB-). Discriminant analysis and PLS-DA have been used to model the passive diffusion component of BBB permeation and potential physicochemical requirement of P-gp substrates.

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