scholarly journals Pregnane X receptors regulate CYP2C8 and P-glycoprotein to impact on the resistance of NSCLC cells to Taxol

2016 ◽  
Vol 5 (12) ◽  
pp. 3564-3571 ◽  
Author(s):  
Yan Chen ◽  
Wandan Huang ◽  
Feiyu Chen ◽  
Guoping Hu ◽  
Fenglei Li ◽  
...  
Keyword(s):  
P Glycoprotein ◽  
Pregnane X Receptors ◽  
X Receptors

In vivo activation of the human CYP3A4 promoter in mouse liver and regulation by pregnane X receptors

2003 ◽  
Vol 65 (11) ◽  
pp. 1889-1896 ◽  
Author(s):  
Weisheng Zhang ◽  
Anthony Purchio ◽  
Kevin Chen ◽  
Stacy M Burns ◽  
Christopher H Contag ◽  
...  
Keyword(s):  
Mouse Liver ◽  
Pregnane X Receptors ◽  
X Receptors

Meclizine ameliorates memory deficits in streptozotocin-induced experimental dementia in mice: role of nuclear pregnane X receptors

2020 ◽  
Vol 98 (6) ◽  
pp. 383-390
Author(s):  
Harmandeep Singh ◽  
Rupinder Kaur Sodhi ◽  
Simerjeet Kaur Chahal ◽  
Jitender Madan
Keyword(s):  
Organic Anion ◽  
Amyloid Β ◽  
Thiobarbituric Acid ◽  
Concomitant Administration ◽  
Morris Water Maze Test ◽  
Histopathological Analysis ◽  
Protective Effects ◽  
Biochemical Alterations ◽  
Pregnane X Receptors ◽  
X Receptors

Pregnane X receptors (PXRs) regulate the expression of ATP-binding cassette proteins transporters and organic anion transporting polypeptides responsible for influx/efflux of xenobiotics across the brain. Ligand activation of PXR augments the expression of P-gp and promotes amyloid-β clearance across the blood–brain barrier. Dementia was induced in mice by intacerebroventricular administration of streptozotocin (STZ) followed by treatment with meclizine, a PXR agonist, and subsequently exposed to the Morris water maze test and biochemical and histopathological analysis to evaluate the effect on cognition. STZ-treated mice exhibited significant enhancement in brain thiobarbituric acid reactive species, interleukin-1β, tumour necrosis factor-α, myeloperoxidase, and acetylcholinestrase activity in addition to diminution in glutathione levels and superoxide dismutase activity in comparison to untreated mice. Administration of meclizine to STZ mice recuperated cognition and biochemical alterations. Concomitant administration of ketoconazole, a PXR antagonist, with meclizine prevented the protective effects. The upshots of our study proclaim that meclizine protects cognitive deficits by virtue of its antioxidant, anticholinesterase, and antiinflammatory properties. Results also signify the potential of PXR in neuroprotective actions of meclizine in dementia.

scholarly journals Liver x receptor alpha drives chemoresistance in response to side-chain hydroxycholesterols in triple negative breast cancer

2020 ◽  
Author(s):  
Samantha A Hutchinson ◽  
Alex Websdale ◽  
Giorgia Cioccoloni ◽  
Hanne Røberg-Larsen ◽  
Priscilia Lianto ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Triple Negative Breast Cancer ◽  
Poor Prognosis ◽  
Triple Negative ◽  
Chemotherapy Resistance ◽  
Resistance Mechanism ◽  
P Glycoprotein ◽  
Tumor Tissues ◽  
X Receptors ◽  
Necessary And Sufficient

AbstractTriple negative breast cancer (TNBC) is challenging to treat successfully because targeted therapies do not exist. Instead, systemic therapy is typically restricted to cytotoxic chemotherapy, which fails more often in patients with elevated circulating cholesterol. Liver x receptors are ligand-dependent transcription factors that are homeostatic regulators of cholesterol, and are linked to regulation of broad-affinity xenobiotic transporter activity in non-tumor tissues. We show that LXR ligands confer chemotherapy resistance in TNBC cell lines and xenografts, and that LXRalpha is necessary and sufficient to mediate this resistance. Furthermore, in TNBC patients who had cancer recurrences, LXRalpha and ligands were independent markers of poor prognosis and correlated with P-glycoprotein expression. However, in patients who survived their disease, LXRalpha signaling and P-glycoprotein were decoupled. These data reveal a novel chemotherapy resistance mechanism in this poor prognosis subtype of breast cancer. We conclude that systemic chemotherapy failure in some TNBC patients is caused by co-opting the LXRalpha:P-glycoprotein axis, a pathway highly targetable by therapies that are already used for prevention and treatment of other diseases.

scholarly journals The Cholesterol-Raising Factor from Coffee Beans, Cafestol, as an Agonist Ligand for the Farnesoid and Pregnane X Receptors

2007 ◽  
Vol 21 (7) ◽  
pp. 1603-1616 ◽  
Author(s):  
Marie-Louise Ricketts ◽  
Mark V. Boekschoten ◽  
Arja J. Kreeft ◽  
Guido J. E. J. Hooiveld ◽  
Corina J. A. Moen ◽  
...  
Keyword(s):  
Coffee Beans ◽  
Pregnane X Receptors ◽  
X Receptors

Characterization of ligand-dependent activation of bovine and pig constitutive androstane (CAR) and pregnane X receptors (PXR) with interspecies comparisons

Xenobiotica ◽  
2015 ◽  
Vol 46 (3) ◽  
pp. 200-210 ◽  
Author(s):  
Jenni Küblbeck ◽  
Vanessa Zancanella ◽  
Viktoria Prantner ◽  
Ferdinand Molnár ◽  
E. James Squires ◽  
...  
Keyword(s):  
Pregnane X Receptors ◽  
X Receptors

scholarly journals Byakangelicin induces cytochrome P450 3A4 expression via transactivation of pregnane X receptors in human hepatocytes

2010 ◽  
Vol 162 (2) ◽  
pp. 441-451 ◽  
Author(s):  
Jian Yang ◽  
Xiaofei Luan ◽  
Haiyan Gui ◽  
Peng Yan ◽  
Dongfang Yang ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Human Hepatocytes ◽  
Cytochrome P450 3A4 ◽  
Pregnane X Receptors ◽  
X Receptors

scholarly journals Schisandrol B protects against cholestatic liver injury through pregnane X receptors

2017 ◽  
Vol 174 (8) ◽  
pp. 672-688 ◽  
Author(s):  
Hang Zeng ◽  
Yiming Jiang ◽  
Pan Chen ◽  
Xiaomei Fan ◽  
Dongshun Li ◽  
...  
Keyword(s):  
Liver Injury ◽  
Pregnane X Receptors ◽  
X Receptors ◽  
Cholestatic Liver Injury

Estrogen, aryl hysdrocarbon and pregnane X receptors activities in reclaimed water and irrigated soils in Oued Souhil area (Nabeul, Tunisia)

Desalination ◽  
2009 ◽  
Vol 246 (1-3) ◽  
pp. 425-434 ◽  
Author(s):  
Olfa Mahjoub ◽  
Marie Leclercq ◽  
Morgane Bachelot ◽  
Claude Casellas ◽  
Aurélie Escande ◽  
...  
Keyword(s):  
Reclaimed Water ◽  
Pregnane X Receptors ◽  
X Receptors ◽  
Irrigated Soils
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