Dual conformation of the ligand induces the partial agonistic activity of retinoid X receptor α (RXRα)
Sign Up to like & getrecommendations! Published in 2019 at "FEBS Letters"
DOI: 10.1002/1873-3468.13301
Abstract: 1‐[(3,5,5,8,8‐pentamethyl‐5,6,7,8‐tetrahydronaphthalen‐2‐yl)amino]benzotriazole‐5‐carboxylic acid (CBt‐PMN), a partial agonist of retinoid X receptor (RXR), has attracted attention due to its potential to treat type 2 diabetes and central nervous system diseases with reduced adverse effects of existing full… read more here.
Keywords: ligand; conformation; receptor rxr; conformation ligand ... See more keywords
Remyelination in humans due to a retinoid‐X receptor agonist is age‐dependent
Sign Up to like & getrecommendations! Published in 2022 at "Annals of Clinical and Translational Neurology"
DOI: 10.1002/acn3.51595
Abstract: Remyelination efficiency declines with advancing age in animal models, but this has been harder to demonstrate in people with multiple sclerosis. We show that bexarotene, a putatively remyelinating retinoid‐X receptor agonist, shortened the visual evoked… read more here.
Keywords: remyelination; age; retinoid receptor; remyelination humans ... See more keywords
Antagonist-perturbation mechanism for activation function-2 fixed motifs: active conformation and docking mode of retinoid X receptor antagonists
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Computer-Aided Molecular Design"
DOI: 10.1007/s10822-017-0025-6
Abstract: HX531, which contains a dibenzodiazepine skeleton, is one of the first retinoid X receptor (RXR) antagonists. Functioning via RXR-PPARγ heterodimer, this compound is receiving a lot of attention as a therapeutic drug candidate for diabetic… read more here.
Keywords: function fixed; docking mode; active conformation; retinoid receptor ... See more keywords
Functional characterization of retinoid X receptor with an emphasis on the mediation of organotin poisoning in the Pacific oyster (Crassostrea gigas).
Sign Up to like & getrecommendations! Published in 2020 at "Gene"
DOI: 10.1016/j.gene.2020.144780
Abstract: Marine mollusks suffer harmful effects due to environmental organotin compounds such as tributyltin (TBT) and triphenyltin (TPT). It is known that gastropod imposex caused by organotins is mediated by a key nuclear receptor, retinoid X… read more here.
Keywords: oyster crassostrea; pacific oyster; crassostrea gigas; receptor ... See more keywords
Increased Molecular Flexibility Widens the Gap between K i and K d values in Screening for Retinoid X Receptor Modulators.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.1c00575
Abstract: Screening for small-molecule modulators targeting a particular receptor is frequently based on measurement of K d, i.e., the binding constant between the receptor and the compound of interest. However, K d values also reflect binding… read more here.
Keywords: retinoid receptor; increased molecular; molecular flexibility; flexibility widens ... See more keywords
The phosphorylated retinoid X receptor-α promotes diethylnitrosamine-induced hepatocarcinogenesis in mice through the activation of β-catenin signaling pathway.
Sign Up to like & getrecommendations! Published in 2021 at "Carcinogenesis"
DOI: 10.1093/carcin/bgab099
Abstract: Previous studies have shown that phosphorylation of the retinoid X receptor-α (RXRα) is associated with the development of hepatocellular carcinoma (HCC). However, these findings were revealed using HCC cell lines that express phosphorylated-RXRα (p-RXRα) proteins;… read more here.
Keywords: catenin; mice; activation; hepatocarcinogenesis ... See more keywords
Transcriptional control of nucleus accumbens neuronal excitability by retinoid X receptor alpha tunes sensitivity to drug rewards
Sign Up to like & getrecommendations! Published in 2022 at "Neuron"
DOI: 10.1101/2022.03.28.486101
Abstract: The complex nature of the transcriptional networks underlying addictive behaviors suggests intricate cooperation between diverse gene regulation mechanisms that go beyond canonical activity-dependent pathways. Here we implicate in this process a novel nuclear receptor transcription… read more here.
Keywords: retinoid receptor; receptor alpha; drug; receptor ... See more keywords
Endogenous retinoid X receptor ligands in mouse hematopoietic cells
Sign Up to like & getrecommendations! Published in 2017 at "Science Signaling"
DOI: 10.1126/scisignal.aan1011
Abstract: The long-chain fatty acid C24:5 is likely an endogenous ligand of the retinoid X receptor α in mouse hematopoietic cells. Endogenous RXRA ligands in hematopoietic cells Like other nuclear receptors, retinoid X receptor α (RXRA)… read more here.
Keywords: reporter; mouse hematopoietic; rxra; retinoid receptor ... See more keywords
Silencing Retinoid X Receptor Alpha Expression Enhances Early-Stage Hepatitis B Virus Infection In Cell Cultures
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Virology"
DOI: 10.1128/jvi.01771-17
Abstract: ABSTRACT Multiple steps of the life cycle of hepatitis B virus (HBV) are known to be coupled to hepatic metabolism. However, the details of involvement of the hepatic metabolic milieu in HBV infection remain incompletely… read more here.
Keywords: receptor alpha; infection; virus; hbv infection ... See more keywords
Effects of electroacupuncture and the retinoid X receptor (RXR) signalling pathway on oligodendrocyte differentiation in the demyelinated spinal cord of rats
Sign Up to like & getrecommendations! Published in 2017 at "Acupuncture in Medicine"
DOI: 10.1136/acupmed-2016-011134
Abstract: Objectives In spinal cord demyelination, some oligodendrocyte precursor cells (OPCs) remain in the demyelinated region but have a reduced capacity to differentiate into oligodendrocytes. This study investigated whether ‘Governor Vessel’ (GV) electroacupuncture (EA) would promote… read more here.
Keywords: cord; group; differentiation; retinoid receptor ... See more keywords
MiRNAs are Unlikely to be Involved in Retinoid Receptor Gene Regulation in Pancreatic Cancer Cells
Sign Up to like & getrecommendations! Published in 2017 at "Cellular Physiology and Biochemistry"
DOI: 10.1159/000485276
Abstract: Background/Aims: Retinoid receptors and retinoic acid were reported to be down-regulated in pancreatic duct adenocarcinoma (PDAC) compared to normal pancreas. Yet the mechanism of the down-regulation of retinoid receptors is not well defined. The aim… read more here.
Keywords: pdac; retinoid receptors; mirnas unlikely; retinoid receptor ... See more keywords