63 research outputs found
MĂ©thodologie gĂ©nĂ©rale dâune Ă©tude ACP : GĂ©nĂ©ralitĂ©s, concepts et exemples
Le dĂ©veloppement des modĂšles statistiques des relations quantitatives structure-activitĂ©/propriĂ©tĂ© joue un rĂŽle important dans la conception de nouveaux produits chimiques spĂ©cialement pharmaceutiques. La prĂ©diction des propriĂ©tĂ©s biologiques des produits non testĂ©es passe dâabord par une analyse ACP. Il sâagit de lâanalyse en composante principale : câest une mĂ©thode basĂ©e sur des statistiques descriptives multidimensionnelles permettant de traiter simultanĂ©ment un nombre quelconque de variables quantitatives. Lâobjectif est de visualiser et rĂ©sumer lâinformation contenue dans les diffĂ©rentes donnĂ©es afin dâavoir une reprĂ©sentation permettant plus facilement lâinterprĂ©tation. Dans ce papier, nous dĂ©crivons des gĂ©nĂ©ralitĂ©s et les principaux concepts et techniques les plus pertinents pour la rĂ©alisation dâune Ă©tude ACP
Tomato SR/CAMTA transcription factors SlSR1 and SlSR3L negatively regulate disease resistance response and SlSR1L positively modulates drought stress tolerance
Bioluminescent kinase strips: A novel approach to targeted and flexible kinase inhibitor profiling
AbstractIn addition to target efficacy, drug safety is a major requirement during the drug discovery process and is influenced by target specificity. Therefore, it is imperative that every new drug candidate be profiled against various liability panels that include protein kinases. Here, an effective methodology to streamline kinase inhibitor profiling is described. An accessible standardized profiling system for 112 protein kinases covering all branches of the kinome was developed. This approach consists of creating different sets of kinases and their corresponding substrates in multi-tube strips. The kinase stocks are pre-standardized for optimal kinase activity and used for inhibitor profiling using a bioluminescent ADP detection assay. We show that these strips can routinely generate inhibitor selectivity profiles for small or broad kinase family panels. Lipid kinases were also assembled in strip format and profiled together with protein kinases. We identified two specific PI3K inhibitors that have off-target effects on CK2 that were not reported before and would have been missed if compounds were not profiled against lipid and protein kinases simultaneously. To validate the accuracy of the data generated by this method, we confirmed that the inhibition potencies observed are consistent with published values produced by more complex technologies such as radioactivity assays
Caracterização de ER49, um fator de elongação da sĂntese de proteĂnas do tipo Ts, expresso durante a maturação do fruto de tomate
The Multiplicity of Polypeptide GalNAcâTransferase: Assays, Inhibitors, and Structures
A Rapid and Efficient Luminescence-based Method for Assaying Phosphoglycosyltransferase Enzymes
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