Strategies for developing pregnane X receptor antagonists: Implications from metabolism to cancer
Sign Up to like & getrecommendations! Published in 2019 at "Medicinal Research Reviews"
DOI: 10.1002/med.21648
Abstract: Pregnane X receptor (PXR) is a ligand‐activated nuclear receptor (NR) that was originally identified as a master regulator of xenobiotic detoxification. It regulates the expression of drug‐metabolizing enzymes and transporters to control the degradation and… read more here.
Keywords: metabolism; drug; pxr; pregnane receptor ... See more keywords
Human pregnane X receptor is activated by dibenzazepine carbamate-based inhibitors of constitutive androstane receptor
Sign Up to like & getrecommendations! Published in 2017 at "Archives of Toxicology"
DOI: 10.1007/s00204-017-1948-3
Abstract: Unintentional activation of xenosensing nuclear receptors pregnane X receptor (PXR) and/or constitutive androstane receptor (CAR) by clinical drug use is known to produce severe side effects in patients, which may be overcome by co-administering antagonists.… read more here.
Keywords: pregnane receptor; dibenzazepine carbamate; pxr; receptor ... See more keywords
Expression dynamics of pregnane X receptor-controlled genes in 3D primary human hepatocyte spheroids.
Sign Up to like & getrecommendations! Published in 2021 at "Archives of toxicology"
DOI: 10.1007/s00204-021-03177-y
Abstract: The pregnane X receptor (PXR) is a ligand-activated nuclear receptor controlling hepatocyte expression of numerous genes. Although expression changes in xenobiotic-metabolizing, lipogenic, gluconeogenic and bile acid synthetic genes have been described after PXR activation, the… read more here.
Keywords: controlled genes; expression; pxr; receptor ... See more keywords
Identification of novel pregnane X receptor (PXR) agonists by In silico and biological activity analyses and reversal of cigarette smoke-induced PXR downregulation.
Sign Up to like & getrecommendations! Published in 2021 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2021.02.145
Abstract: Cigarette smoke (CS) contains many toxins that collectively harm nearly every organ in the body, and smoking is a key risk factor for many chronic diseases. Aside from its toxic actions, CS may alter expression… read more here.
Keywords: receptor pxr; cigarette smoke; pxr; pregnane receptor ... See more keywords
Epigenetic sensitization of Pregnane X Receptor-regulated gene expression by dimethyl sulfoxide.
Sign Up to like & getrecommendations! Published in 2019 at "Toxicology letters"
DOI: 10.1016/j.toxlet.2019.12.029
Abstract: Prior exposures to chemicals/agents may alter epigenome in such a way that subsequent exposure to the same or different xenobiotic would produce different responses. Understanding the mechanism for this "priming" effect is of clinical significance… read more here.
Keywords: pregnane receptor; dimethyl sulfoxide; gene; effect ... See more keywords
Pregnane X Receptor Activation in Liver Perfusion.
Sign Up to like & getrecommendations! Published in 2022 at "Transplantation proceedings"
DOI: 10.1016/j.transproceed.2021.12.044
Abstract: BACKGROUND Liver normothermic machine perfusion (NMP) is being adopted as a method of optimizing livers before transplantation. However, there is further potential to use the NMP model as a platform for drug delivery. Pregnane X… read more here.
Keywords: activation; perfusion; pregnane receptor; drug delivery ... See more keywords
Alismanin A, a Triterpenoid with a C34 Skeleton from Alisma orientale as a Natural Agonist of Human Pregnane X Receptor.
Sign Up to like & getrecommendations! Published in 2017 at "Organic letters"
DOI: 10.1021/acs.orglett.7b02738
Abstract: Alismanin A (1), a novel aromatic triterpenoid with a C34 skeleton, was isolated from Alisma orientale together with a rearranged nor-triterpenoid (2) and a 13,17-seco triterpenoid (3). Their structures were determined by a combination of… read more here.
Keywords: triterpenoid c34; c34 skeleton; alisma orientale; pregnane receptor ... See more keywords
Overcoming the Pregnane X Receptor Liability: Rational Design to Eliminate PXR-Mediated CYP Induction.
Sign Up to like & getrecommendations! Published in 2021 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.1c00187
Abstract: The pregnane X receptor (PXR) regulates expression of proteins responsible for all three phases required for the detoxification mechanism, which include CYP450 enzymes, phase II enzymes, and multidrug efflux pumps. Therefore, PXR is a prominent… read more here.
Keywords: chemistry; drug; pxr; receptor ... See more keywords
Non-genomic effects of the Pregnane X Receptor negatively regulate platelet functions, thrombosis and haemostasis
Sign Up to like & getrecommendations! Published in 2019 at "Scientific Reports"
DOI: 10.1038/s41598-019-53218-x
Abstract: The pregnane X receptor (PXR) is a nuclear receptor (NR), involved in the detoxification of xenobiotic compounds. Recently, its presence was reported in the human vasculature and its ligands were proposed to exhibit anti-atherosclerotic effects.… read more here.
Keywords: pregnane receptor; platelet functions; receptor; platelet ... See more keywords
Suppression of carboxylesterases by imatinib mediated by the down‐regulation of pregnane X receptor
Sign Up to like & getrecommendations! Published in 2017 at "British Journal of Pharmacology"
DOI: 10.1111/bph.13731
Abstract: Imatinib mesylate (IM) is a first‐line treatment for chronic myeloid leukaemia (CML) as a specific inhibitor of BCR‐ABL tyrosine kinase. As IM is widely used in CML, in combination with other drugs, the effects of… read more here.
Keywords: regulation pregnane; mediated regulation; carboxylesterases imatinib; imatinib mediated ... See more keywords
The association of pregnane X receptor activation with outcomes after liver transplantation—A retrospective study
Sign Up to like & getrecommendations! Published in 2019 at "Clinical Transplantation"
DOI: 10.1111/ctr.13734
Abstract: Many complications following liver transplantation are linked to ischemia‐reperfusion injury. Activation of the pregnane X receptor (PXR) has been shown to alleviate this process in animal models. The aim of this retrospective study was to… read more here.
Keywords: liver transplantation; transplantation; activation; pregnane receptor ... See more keywords