Natural and synthetic retinoid X receptor ligands and their role in selected nuclear receptor action
Language English Country France Media print-electronic
Document type Journal Article, Review
PubMed
33011201
DOI
10.1016/j.biochi.2020.09.027
PII: S0300-9084(20)30257-1
Knihovny.cz E-resources
- Keywords
- Human microbiota, Ligand inducible transcription factors, Natural and synthetic RXR ligands, Nuclear receptors, Retinoid X receptors (RXR),
- MeSH
- Humans MeSH
- Ligands MeSH
- Microbiota MeSH
- Organotin Compounds pharmacology MeSH
- Receptors, Cytoplasmic and Nuclear physiology MeSH
- Retinoid X Receptors agonists physiology MeSH
- Tretinoin analogs & derivatives metabolism MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Review MeSH
- Names of Substances
- Ligands MeSH
- Organotin Compounds MeSH
- Receptors, Cytoplasmic and Nuclear MeSH
- Retinoid X Receptors MeSH
- Tretinoin MeSH
Important key players in the regulatory machinery within the cells are nuclear retinoid X receptors (RXRs), which compose heterodimers in company with several diverse nuclear receptors, playing a role as ligand inducible transcription factors. In general, nuclear receptors are ligand-activated, transcription-modulating proteins affecting transcriptional responses in target genes. RXR molecules forming permissive heterodimers with disparate nuclear receptors comprise peroxisome proliferator-activated receptors (PPARs), liver X receptors (LXRs), farnesoid X receptor (FXR), pregnane X receptor (PXR) and constitutive androstan receptor (CAR). Retinoid receptors (RARs) and thyroid hormone receptors (TRs) may form conditional heterodimers, and dihydroxyvitamin D3 receptor (VDR) is believed to form nonpermissive heterodimer. Thus, RXRs are the important molecules that are involved in control of many cellular functions in biological processes and diseases, including cancer or diabetes. This article summarizes both naturally occurring and synthetic ligands for nuclear retinoid X receptors and describes, predominantly in mammals, their role in molecular mechanisms within the cells. A focus is also on triorganotin compounds, which are high affinity RXR ligands, and finally, we present an outlook on human microbiota as a potential source of RXR activators. Nevertheless, new synthetic rexinoids with better retinoid X receptor activity and lesser side effects are highly required.
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