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A study of ligand-binding properties of Hepatocyte Nuclear Factor 4α: A study of the ligand-binding properties of Hepatocyte Nuclear Factor 4α, using a DAUDA fluorescence displacement assay - Couverture souple

Papachristodoulou, Maria; Thumser, Alfred; Plant, Nick

 
9783846580820: A study of ligand-binding properties of Hepatocyte Nuclear Factor 4α: A study of the ligand-binding properties of Hepatocyte Nuclear Factor 4α, using a DAUDA fluorescence displacement assay
Couverture souple
ISBN 10 : 3846580821 ISBN 13 : 9783846580820
Editeur : LAP LAMBERT Academic Publishing, 2012

Synopsis

Hepatocyte nuclear factor 4α (HNF4α) is a liver enriched transcription factor that belongs to the nuclear receptor family, and controls the expression of genes involved in various different functions, such as nutrient transport, metabolism, growth and differentiation. Recently, fatty acids and/or fatty acyl CoAs as well as some xenobiotics (e.g. hypolipidemic drugs) have been suggested as HNF4α ligands. The aim of this study was to identify potential ligands for HNF4α, using a DAUDA fluorescence displacement assay. LFABP was expressed and purified as a positive control, and used successfully to validate the DAUDA assay. Rat HNF4αLBD was successfully expressed and purified, therefore further work for ligand identification was performed using the rat HNF4α. Suitability of the DAUDA fluorescence displacement assay for screening of ligands for rat HNF4α was confirmed by a characteristic blue shift in fluorescence emission upon protein binding, as previously reported. Ligands screened in this study included five different fatty acids, palmitoyl CoA, and hypolipidemic xenobiotics of the fibrate family (fenofibrate, bezafibrate, clofibrate), as well as pioglitazone (a thionolidinedione).

Les informations fournies dans la section « Synopsis » peuvent faire référence à une autre édition de ce titre.

Présentation de l'éditeur

Hepatocyte nuclear factor 4α (HNF4α) is a liver enriched transcription factor that belongs to the nuclear receptor family, and controls the expression of genes involved in various different functions, such as nutrient transport, metabolism, growth and differentiation. Recently, fatty acids and/or fatty acyl CoAs as well as some xenobiotics (e.g. hypolipidemic drugs) have been suggested as HNF4α ligands. The aim of this study was to identify potential ligands for HNF4α, using a DAUDA fluorescence displacement assay. LFABP was expressed and purified as a positive control, and used successfully to validate the DAUDA assay. Rat HNF4αLBD was successfully expressed and purified, therefore further work for ligand identification was performed using the rat HNF4α. Suitability of the DAUDA fluorescence displacement assay for screening of ligands for rat HNF4α was confirmed by a characteristic blue shift in fluorescence emission upon protein binding, as previously reported. Ligands screened in this study included five different fatty acids, palmitoyl CoA, and hypolipidemic xenobiotics of the fibrate family (fenofibrate, bezafibrate, clofibrate), as well as pioglitazone (a thionolidinedione).

Biographie de l'auteur

Maria Papachristodoulou (BSc Hons, MPhil,University of Surrey, UK) is a Biology teacher in Cyprus. Dr Alfred Thumser (PhD,University of Cape Town) is a Lecturer in Biochemistry at the University of Surrey. Dr Nick Plant (PhD, University of Nottingham, UK) is a Senior Lecturer in Molecular Toxicology at the University of Surrey.

Les informations fournies dans la section « A propos du livre » peuvent faire référence à une autre édition de ce titre.

Éditeur
LAP LAMBERT Academic Publishing
Date d'édition
2012
Langue
anglais
ISBN 10 
3846580821
ISBN 13 
9783846580820
Reliure
Broché
Nombre de pages
220
Coordonnées du fabricant
non disponible
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