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  • Title: Development of a profiling strategy for metabolic mixtures by combining chromatography and mass spectrometry with cell-based GPCR signaling.
    Author: Nijmeijer S, Vischer HF, Rudebeck AF, Fleurbaaij F, Falck D, Leurs R, Niessen WM, Kool J.
    Journal: J Biomol Screen; 2012 Dec; 17(10):1329-38. PubMed ID: 22740245.
    Abstract:
    In this study, we developed an in-line methodology that combines analytical with pharmacological techniques to characterize metabolites of human histamine H(4) receptor (hH(4)R) ligands. Liquid chromatographic separation of metabolic mixtures is coupled to high-resolution fractionation into 96- or 384-well plates and directly followed by a cell-based reporter gene assay to measure receptor signaling. The complete methodology was designed, optimized, validated, and ultimately miniaturized into a high-density well plate format. Finally, the methodology was demonstrated in a metabolic profiling setting for three hH(4)R lead compounds and the drug clozapine. This new methodology comprises integrated analytical separations, mass spectrometry, and a cell-based signal transduction-driven reporter gene assay that enables the implementation of comprehensive metabolic profiling earlier in the drug discovery process.
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