An optimized protocol with a stepwise ...
Document type :
Compte-rendu et recension critique d'ouvrage
Title :
An optimized protocol with a stepwise approach to identify specific nuclear receptor ligands from cultured mammalian cells
Author(s) :
Berthier, Alexandre [Auteur]
Récepteurs Nucléaires, Maladies Métaboliques et Cardiovasculaires - U1011 [RNMCD]
Staels, Bart [Auteur]
Récepteurs Nucléaires, Maladies Métaboliques et Cardiovasculaires - U1011 [RNMCD]
Lefebvre, Philippe [Auteur correspondant]
Récepteurs Nucléaires, Maladies Métaboliques et Cardiovasculaires - U1011 [RNMCD]
Récepteurs Nucléaires, Maladies Métaboliques et Cardiovasculaires - U1011 [RNMCD]
Staels, Bart [Auteur]
Récepteurs Nucléaires, Maladies Métaboliques et Cardiovasculaires - U1011 [RNMCD]
Lefebvre, Philippe [Auteur correspondant]
Récepteurs Nucléaires, Maladies Métaboliques et Cardiovasculaires - U1011 [RNMCD]
Journal title :
STAR Protocols
Pages :
100658
Publisher :
Elsevier
Publication date :
2021-09-17
ISSN :
2666-1667
English keyword(s) :
Circadian rhythm
Liver
PPARs
Physiology
Sexual dimorphism
Zonation
Liver
PPARs
Physiology
Sexual dimorphism
Zonation
HAL domain(s) :
Sciences du Vivant [q-bio]
English abstract : [en]
Here, we describe an optimized protocol to identify specific nuclear receptor ligands. First, to rule out any compound interference with luciferase activity per se, we describe an in vitro assay assessing potential inhibition ...
Show more >Here, we describe an optimized protocol to identify specific nuclear receptor ligands. First, to rule out any compound interference with luciferase activity per se, we describe an in vitro assay assessing potential inhibition or activation of luciferase enzymatic activity. Second, to comply with EMA and FDA guidelines to mitigate drug-drug interactions, we detail assays assessing CAR and PXR activation ability. Finally, to minimize off-target detection effects, we describe the use of mammalian one-(or two-) hybrid systems. For complete details on the use and execution of this protocol, please refer to Hering et al. (2018).Show less >
Show more >Here, we describe an optimized protocol to identify specific nuclear receptor ligands. First, to rule out any compound interference with luciferase activity per se, we describe an in vitro assay assessing potential inhibition or activation of luciferase enzymatic activity. Second, to comply with EMA and FDA guidelines to mitigate drug-drug interactions, we detail assays assessing CAR and PXR activation ability. Finally, to minimize off-target detection effects, we describe the use of mammalian one-(or two-) hybrid systems. For complete details on the use and execution of this protocol, please refer to Hering et al. (2018).Show less >
Language :
Anglais
Popular science :
Non
ANR Project :
Source :
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