Results 71 to 80 of about 12,669 (162)

The Blood–Brain Barrier as an Integration Hub in Alzheimer's Disease: How Microbiota Metabolites Modulate Central Signal Processing

CNS Neuroscience &Therapeutics, Volume 31, Issue 12, December 2025.
The review reframes the blood–brain barrier as an active integrator of microbiota‐derived signals that shape vulnerability to Alzheimer's disease. Viewing the BBB as a dynamic processing interface between gut and brain clarifies why identical metabolite patterns yield different outcomes and opens new opportunities for earlier diagnosis and targeted ...
O. Giangiulio, R. Maccarone
wiley   +1 more source

Novel functions of PXR in cardiometabolic disease [PDF]

Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms, 2016
Cardiometabolic disease emerges as a worldwide epidemic and there is urgent need to understand the molecular mechanisms underlying this chronic disease. The chemical environment to which we are exposed has significantly changed in the past few decades and recent research has implicated its contribution to the development of many chronic human diseases.
openaire   +2 more sources

Advancing Predictions of Oral Drug Absorption, CYP3A4 Induction, and Transporter‐Mediated Interactions Using a Human Primary Intestinal 3D Model (EpiIntestinal™)

Clinical Pharmacology &Therapeutics, Volume 118, Issue 6, Page 1499-1511, December 2025.
Accurate prediction of oral drug absorption in humans is essential for early drug development; however, physiologically relevant human models are lacking. This study aims to comprehensively assess the EpiIntestinal™, a human primary intestinal 3D model, for its ability to predict oral absorption (Fa), intestinal availability (Fg), CYP3A4 induction, and
Paresh P. Chothe, Andrea Whitcher‐Johnstone, Aniruddha Karve, Diane Ramsden, Niresh Hariparsad   +4 more
wiley   +1 more source

S-nitrosylation attenuates pregnane X receptor hyperactivity and acetaminophen-induced liver injury

JCI Insight
Drug-induced liver injury (DILI), especially acetaminophen overdose, is the leading cause of acute liver failure. Pregnane X receptor (PXR) is a nuclear receptor and the master regulator of drug metabolism.
Qi Cui, Tingting Jiang, Xinya Xie, Haodong Wang, Lei Qian, Yanyan Cheng, Qiang Li, Tingxu Lu, Qinyu Yao, Jia Liu, Baochang Lai, Chang Chen, Lei Xiao, Nanping Wang   +13 more
doaj   +1 more source

Nuclear receptor PXR, transcriptional circuits and metabolic relevance

Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease, 2011
The pregnane X receptor (PXR, NR1I2) is a ligand activated transcription factor that belongs to the nuclear hormone receptor (NR) superfamily. PXR is highly expressed in the liver and intestine, but low levels of expression have also been found in many other tissues.
Ihunnah, Chibueze A., Jiang, Mengxi, Xie, Wen   +2 more
openaire   +3 more sources

Pregnane X receptor is associated with unfavorable survival and induces chemotherapeutic resistance by transcriptional activating multidrug resistance-related protein 3 in colorectal cancer

Molecular Cancer, 2017
Background Although chemotherapy represents a predominant anti-cancer therapeutic modality, drug treatment efficacy is often limited due to the development of resistant tumor cells.
Yan Dong, Zhe Wang, Gan-feng Xie, Chong Li, Wen-wei Zuo, Gang Meng, Cheng-ping Xu, Jian-jun Li   +7 more
doaj   +1 more source

A Population Pharmacokinetic Approach to Understand the Effect of Efavirenz on CYP3A Activity in Healthy Volunteers Using Midazolam as a Probe

CPT: Pharmacometrics &Systems Pharmacology, Volume 14, Issue 12, Page 2095-2106, December 2025.
ABSTRACT Efavirenz induces and inhibits multiple drug‐metabolizing enzymes, contributing to significant drug–drug interactions. This study quantified the impact of multiple doses of efavirenz on CYP3A activity via midazolam metabolism using a population pharmacokinetic approach.
Kimberly S. Collins, Blessed W. Aruldhas, Ingrid F. Metzger, Jessica B. L. Lu, Michael A. Heathman, Sara K. Quinney, Zeruesenay Desta   +6 more
wiley   +1 more source

Pregnane X receptor activation constrains mucosal NF-κB activity in active inflammatory bowel disease.

PLoS ONE, 2019
BACKGROUND:The Pregnane X Receptor (PXR) is a principal signal transducer in mucosal responses to xenobiotic stress. It is well-recognized that inflammatory bowel disease is accompanied by xenobiotic stress, but the importance of the PXR in limiting ...
J Jasper Deuring, Meng Li, Wanlu Cao, Sunrui Chen, Wenshi Wang, Colin de Haar, C Janneke van der Woude, Maikel Peppelenbosch   +7 more
doaj   +1 more source

Pregnane X receptor (PXR)-mediated gene repression and cross-talk of PXR with other nuclear receptors via coactivator interactions

Frontiers in Pharmacology, 2016
Pregnane X receptor is a ligand-activated nuclear receptor that mainly controls inducible expression of xenobiotics handling genes including biotransformation enzymes and drug transporters.
Petr Pavek
doaj   +1 more source

Targeting the pregnane X receptor using microbial metabolite mimicry

EMBO Molecular Medicine, 2020
The human PXR (pregnane X receptor), a master regulator of drug metabolism, has essential roles in intestinal homeostasis and abrogating inflammation. Existing PXR ligands have substantial off‐target toxicity.
Zdeněk Dvořák, Felix Kopp, Cait M Costello, Jazmin S Kemp, Hao Li, Aneta Vrzalová, Martina Štěpánková, Iveta Bartoňková, Eva Jiskrová, Karolína Poulíková, Barbora Vyhlídalová, Lars U Nordstroem, Chamini V Karunaratne, Harmit S Ranhotra, Kyu Shik Mun, Anjaparavanda P Naren, Iain A Murray, Gary H Perdew, Julius Brtko, Lucia Toporova, Arne Schön, Bret D Wallace, William G Walton, Matthew R Redinbo, Katherine Sun, Amanda Beck, Sandhya Kortagere, Michelle C Neary, Aneesh Chandran, Saraswathi Vishveshwara, Maria M Cavalluzzi, Giovanni Lentini, Julia Yue Cui, Haiwei Gu, John C March, Shirshendu Chatterjee, Adam Matson, Dennis Wright, Kyle L Flannigan, Simon A Hirota, Ryan Balfour Sartor, Sridhar Mani   +41 more
doaj   +1 more source