Modulation of xenobiotic receptors by steroids.

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Banerjee M, Robbins D, Chen T

Modulation of xenobiotic receptors by steroids.

Molecules. 2013 Jun 24;18(7):7389-406. doi: 10.3390/molecules18077389.

PubMed ID

23884115 [ View in PubMed

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Abstract

Nuclear receptors (NRs) are ligand-activated transcription factors that regulate the expression of their target genes. NRs play important roles in many human diseases, including metabolic diseases and cancer, and are therefore a key class of therapeutic targets. Steroids play important roles in regulating nuclear receptors; in addition to being ligands of steroid receptors, steroids (and their metabolites) also regulate other NRs, such as the pregnane X receptor and constitutive androstane receptor (termed xenobiotic receptors), which participate in steroid metabolism. Xenobiotic receptors have promiscuous ligand-binding properties, and their structurally diverse ligands include steroids and their metabolites. Therefore, steroids, their metabolism and metabolites, xenobiotic receptors, steroid receptors, and the respective signaling pathways they regulate have functional interactions. This review discusses these functional interactions and their implications for activities mediated by steroid receptors and xenobiotic receptors, focusing on steroids that modulate pathways involving the pregnane X receptor and constitutive androstane receptor. The emphasis of the review is on structure-function studies of xenobiotic receptors bound to steroid ligands.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Estradiol	Estrogen receptor alpha	Protein	Humans	Yes	Agonist	Details
Estradiol	Nuclear receptor subfamily 1 group I member 2	Protein	Humans	Unknown	Binder	Details