Destabilization of the torsioned conformation of a ligand side chain inverts the LXRβ activity

Background Liver X receptors (LXRs) are transcription factors activated by cholesterol metabolites containing an oxidized side chain. Due to their ability to regulate lipid metabolism and cholesterol transport, they have become attractive pharmacological targets. LXRs are closely related to DAF-12,...

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Detalles Bibliográficos
Autores principales: Dansey, Maria Virginia, Grinman, Diego Yair, Estrin, Dario Ariel, Veleiro, Adriana Silvia, Pecci, Adali, Burton, Gerardo
Publicado: 2015
Materias:
Cholestenoic acid
Inverse agonism
Liver X receptors
Molecular dynamics
27 nor 5 cholestenoic acid
carboxyl group
cholesterol
ligand
liver X receptor alpha
liver X receptor beta
methyl group
steroid
unclassified drug
cholestane derivative
cholestenoic acid
liver X receptor
orphan nuclear receptor
Article
conformational transition
gene expression
gene expression assay
in vitro study
ligand binding
molecular dynamics
molecular stability
priority journal
protein conformation
reporter gene
simulation
antagonists and inhibitors
binding site
drug effects
gene expression regulation
genetics
HEK293 cell line
HepG2 cell line
human
metabolism
Binding Sites
Cholestenes
Gene Expression Regulation
HEK293 Cells
Hep G2 Cells
Humans
Ligands
Orphan Nuclear Receptors
Acceso en línea:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_13881981_v1851_n12_p1577_Alvarez
http://hdl.handle.net/20.500.12110/paper_13881981_v1851_n12_p1577_Alvarez
Aporte de:
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires

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