Results 111 to 120 of about 45,599 (229)

Nose-to-brain delivery of antiviral drugs: A way to overcome their active efflux? [PDF]

, 2018
Although several viruses can easily infect the central nervous system (CNS), antiviral drugs often show dramatic difficulties in penetrating the brain from the bloodstream since they are substrates of active efflux transporters (AETs). These transporters,
Dalpiaz, Alessandro, Pavan, Barbara
core   +2 more sources

Helix 11 Dynamics Is Critical for Constitutive Androstane Receptor Activity [PDF]

Structure, 2011
The constitutive androstane receptor (CAR) transactivation can occur in the absence of exogenous ligand and this activity is enhanced by agonists TCPOBOP and meclizine. We use biophysical and cell-based assays to show that increased activity of CAR(TCPOBOP) relative to CAR(meclizine) corresponds to a higher affinity of CAR(TCPOBOP) for the steroid ...
Wright, Edward, Busby, Scott A., Wisecarver, Sarah, Vincent, Jeremy, Griffin, Patrick R., Fernandez, Elias J.   +5 more
openaire   +2 more sources

Adiponectin Regulated by Indole‐3‐Acetic Acid in Paneth Cells Controls Renewal and Differentiation of Gut Stem Cells

The FASEB Journal, Volume 39, Issue 19, 15 October 2025.
The adiponectin produced by Paneth cells suppresses intestinal stem cell renewal and differentiation by signaling through adiponectin receptor 1. This inhibitory effect is counterbalanced by gut microbiota‐derived indole‐3‐acetic acid, which activates the pregnane X receptor to downregulate adiponectin expression, consequently enhancing intestinal stem
Hang Liu, Xiaomin Su, Juanjuan Wang, Mengli Jin, Yuan Zhang, Rongcun Yang   +5 more
wiley   +1 more source

Sports Supplement Analysis Survey for the Prevalence of WADA Prohibited Substances in the Australian Online Marketplace

Drug Testing and Analysis, Volume 17, Issue 10, Page 1857-1864, October 2025.
A survey of 200 sports supplements purchased online in Australia and analysed for WADA Prohibited Substances. Athlete education regarding the use of sports supplements remains a high priority as 35% of the products contained WADA Prohibited Substances. ABSTRACT Sports supplements are used extensively by people involved in competitive sports. However, a
Louise Barker, Adam Cawley, Naomi Speers, Kerry Knowler, Karina Chilman   +4 more
wiley   +1 more source

Structure and Function of the Nuclear Receptor Constitutive Androstane Receptor

YAKUGAKU ZASSHI, 2016
Animal defense mechanisms against both endogenous and exogenous toxic compounds function mainly through receptor-type transcription factors, including the constitutive androstane receptor (CAR). Following xenobiotic stimulation, CAR translocates into the nucleus and transactivates its target genes including oxygenic and conjugative enzymes and ...
openaire   +3 more sources

Constitutive androstane receptor regulates the intestinal mucosal response to injury [PDF]

British Journal of Pharmacology, 2017
Background and PurposeThe pathogenesis of the inflammatory bowel diseases (IBD), comprising Crohn's disease (CD) and ulcerative colitis (UC), involves aberrant interactions between a genetically susceptible individual, their microbiota and environmental factors.
Grace M Hudson, Kyle L Flannigan, Sarah L Erickson, Fernando A Vicentini, Alexandra Zamponi, Christina L Hirota, Laurie Alston, Christophe Altier, Subrata Ghosh, Kevin P Rioux, Sridhar Mani, Thomas K Chang, Simon A Hirota   +12 more
openaire   +2 more sources

A gut microbiota‐bile acid axis inhibits the infection of an emerging coronavirus by targeting its cellular receptor aminopeptidase N

iMeta, Volume 4, Issue 5, October 2025.
Bacteroides fragilis employs bile salt hydrolase to reprogram host bile acid metabolism, generating lithocholic acid that directly blocks porcine deltacoronavirus infection by disrupting spike protein‐aminopeptidase N binding, defining a microbiota‐bile acid antiviral axis with therapeutic potential against coronaviruses.
Ya‐Qing Zhang, Bin Wang, Yong‐Le Yang, Jin‐Xin Meng, Meng‐Di Zhang, Yi‐Ke Li, Bo Dong, Yanan Zhang, Bo‐Wen Liu, Dong Yang, Chun‐Miao Ji, Yao‐Wei Huang, Shu Jeffrey Zhu   +12 more
wiley   +1 more source

Impact of Parenteral Nutrition Versus Fasting on Hepatic Bile Acid Production and Transport in a Rabbit Model of Prolonged Critical Illness [PDF]

, 1986
Cholestatic liver dysfunction frequently occurs during critical illness. Administration of parenteral nutrition (PN) is thought to aggravate this.
Vanwijngaerden, Yoo-Mee, Langouche, Lies, Derde, Sarah, Liddle, Christopher, Coulter, Sally, Van den Berghe, Greet, Mesotten, Dieter   +6 more
core   +2 more sources

Metamizole induces voriconazole metabolism and results in subtherapeutic voriconazole concentrations

British Journal of Clinical Pharmacology, Volume 91, Issue 9, Page 2598-2604, September 2025.
Aims Voriconazole is extensively metabolized via cytochrome P450 (CYP) enzymes, predominantly CYP2C19 and CYP3A4. Drugs influencing the activity or expression of CYP enzymes can cause clinically relevant changes in the metabolism and voriconazole exposure. Metamizole is known to induce CYP3A4 and CYP2C19.
Simone D. Baan, Daan J. Touw, Marjolijn N. Lub‐de Hooge, Thijs H. Oude Munnink   +3 more
wiley   +1 more source

Regulation of CAR and PXR Expression in Health and Disease

Cells, 2020
Pregnane X receptor (PXR, NR1I2) and constitutive androstane receptor (CAR, NR1I3) are members of the nuclear receptor superfamily that mainly act as ligand-activated transcription factors. Their functions have long been associated with the regulation of
Martine Daujat-Chavanieu, Sabine Gerbal-Chaloin   +1 more
doaj   +1 more source