Titlebook: Optimization in Drug Discovery; In Vitro Methods Gary W. Caldwell,Zhengyin Yan Book 2014Latest edition Springer Science+Business Media New

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HUMP

In Vitro CYP/FMO Reaction Phenotyping, drug might be susceptible to changes in its exposure or to cause changes in the exposure of concomitantly administered drugs. The semi-quantitative assessment of the relative contributions of these pathways can provide early insight to the potential for drug-drug interactions or to possible affinit

发酵剂

Human Pregnane X Receptor (hPXR) Activation Assay in Stable Cell Lines,eractions (DDIs) is a wildly used technique among . assays. Direct assessment of PXR activation is a cell-based assay that requires two major components, the PXR and a reporter gene linked to the promoter and enhancer regions of the CYP3A gene. Because of species differences in the ligand binding re

半导体

Characterization of Constitutive Androstane Receptor (CAR) Activation,ous hepatic drug-metabolizing enzymes and transporters in response to various xenobiotic exposures. Unlike most prototypical nuclear receptors, however, CAR can be activated . both direct ligand-binding and ligand-independent indirect mechanisms. Moreover, whereas CAR predominantly resides in the cy

设施

MOTIF

Cell-Based Assays for Identification of Aryl Hydrocarbon Receptor (AhR) Activators,tructurally diverse synthetic and naturally occurring chemicals. The role of the AhR and its signaling pathway in endogenous physiological functions and its involvement in immune cell development and human diseases has made it a target for development of therapeutic agents. The ability of the AhR to

Estimable

In Vitro CYP Induction Using Human Hepatocytes,ar receptors (NRs), respectively, is routinely determined during small molecule drug development. Significant CYP induction can result in therapeutic failure from clinical exposure of a compound outside the therapeutic window, if the respective enzymes are responsible for a significant portion of th

aristocracy

CLAY

Evaluation of Time-Dependent CYP3A4 Inhibition Using Human Hepatocytes, a clinical interaction from pre-clinical TDI data have been lacking. Although more complex prediction algorithms have been developed, the accuracy has still improved little. This suggests alternate methods to collect input data may improve prediction robustness. Historically, human liver microsomes

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