Results 51 to 60 of about 8,905 (163)

The Effect of Dicloxacillin Administration on Pharmacokinetics of Narrow Therapeutic Window Drugs: Phenytoin and Warfarin

Clinical Pharmacology &Therapeutics, EarlyView.
Dicloxacillin is a penicillinase‐resistant beta‐lactam antibiotic and potent activator of the Pregnane X receptor (PXR), known to induce CYP2C9, CYP2C19, and CYP3A4 activity. Clinical data suggest it reduces anticoagulation in warfarin‐treated patients and increases the risk of thromboembolic events.
Chanan Shaul, Waseem Mujahed, Ibrahim Idries, Maor Wanounou, Meir Bialer, Yoseph Caraco   +5 more
wiley   +1 more source

An optimized protocol with a stepwise approach to identify specific nuclear receptor ligands from cultured mammalian cells

STAR Protocols, 2021
Summary: Here, we describe an optimized protocol to identify specific nuclear receptor ligands. First, to rule out any compound interference with luciferase activity per se, we describe an in vitro assay assessing potential inhibition or activation of ...
Alexandre Berthier, Bart Staels, Philippe Lefebvre   +2 more
doaj   +1 more source

The gut microbiome and drug‐resistant epilepsy: Microbiome–antiseizure medication interactions and implications for pharmacoresistance

Epilepsia Open, EarlyView.
Abstract Drug‐resistant epilepsy (DRE) affects approximately one‐third of patients with epilepsy and represents a major unmet clinical need. While traditional hypotheses of pharmacoresistance have focused on alterations in drug targets, efflux transporter overexpression, and intrinsic disease severity, the gut microbiome has recently emerged as a ...
Khaled Zammar, Majd A. AbuAlrob, Musab Ali, Simona Lattanzi, Boulenouar Mesraoua   +4 more
wiley   +1 more source

The Structural Basis of Pregnane X Receptor Binding Promiscuity [PDF]

Biochemistry, 2009
The steroid and xenobiotic-responsive human pregnane X receptor (PXR) binds a broad range of structurally diverse compounds. The structures of the apo and ligand-bound forms of PXR are very similar, in contrast to most promiscuous proteins that generally adapt their shape to different ligands. We investigated the structural origins of PXR's recognition
Chi-Ho, Ngan, Dmitri, Beglov, Aleksandra N, Rudnitskaya, Dima, Kozakov, David J, Waxman, Sandor, Vajda   +5 more
openaire   +2 more sources

Bile acid metabolism and signaling in human and animal health: A One Health perspective

iMetaOmics, EarlyView.
Bile acids maintain host homeostasis through enterohepatic circulation, microbial transformation, and bile acid receptor signaling, thereby regulating glucose and lipid metabolism, intestinal barrier integrity, and immunity. These effects support human disease intervention and health‐oriented animal production, reducing drug dependence and residue ...
Lei Li, Shuai Liu, Zhijun Cao, Yangchun Cao, Shengru Wu, Lu Deng, Junhu Yao, Jun Zhang   +7 more
wiley   +1 more source

Nuclear Receptors as Targets for Drug Development: Regulation of Cholesterol and Bile Acid Metabolism by Nuclear Receptors

Journal of Pharmacological Sciences, 2005
Nuclear receptors are ligand-dependent transcription factors that recently have been shown to play important roles in the metabolism of cholesterol and bile acids.
Makoto Makishima
doaj   +1 more source

Microbial metabolite indole‐3‐propionic acid preserves astrocytic mitochondrial mitofusin 2 to limit neuroinflammation after traumatic brain injury

Interdisciplinary Medicine, EarlyView.
Following traumatic brain injury, indole‐3‐propionic acid (IPA) directly targets the aryl hydrocarbon receptor on astrocytes in the peri‐lesional cortex; this suppresses interferon regulatory factor 1‐driven transcription of the E3 ubiquitin ligase RFFL (ring finger and FYVE‐like domain containing E3 ubiquitin protein ligase).
Ziwen Zhang, Kai Wang, Liangbo Wang, Wencong Li, Hao Guo, Meng Xu, Tinghao Wang, Jiahui Ren, Ting Zhu, Jiahui Wang, Wenxing Cui, Jinpeng Zhou, Yang Tian, Liying Han, Chengxuan Guo, Shuoyao Ma, Qiang Wang, Zhihong Li, Yaning Cai, Jingyu Dong, Xun Wu, Haixiao Liu, Yan Qu   +22 more
wiley   +1 more source

Pregnane X receptor knockout mice display aging-dependent wearing of articular cartilage.

PLoS ONE, 2015
Steroid and xenobiotic receptor (SXR) and its murine ortholog, pregnane X receptor (PXR), are nuclear receptors that are expressed at high levels in the liver and the intestine where they function as xenobiotic sensors that induce expression of genes ...
Kotaro Azuma, Stephanie C Casey, Tomohiko Urano, Kuniko Horie-Inoue, Yasuyoshi Ouchi, Bruce Blumberg, Satoshi Inoue   +6 more
doaj   +1 more source

Regulation of bile acid receptor activity

Liver Research, 2018
Many receptors can be activated by bile acids (BAs) and their derivatives. These include nuclear receptors farnesoid X receptor (FXR), pregnane X receptor (PXR), and vitamin D receptor (VDR), as well as membrane receptors Takeda G protein receptor 5 ...
Yu-Jui Yvonne Wan, Lili Sheng
doaj   +1 more source

Mode‐of‐Action and Human Relevance Assessment for Diisononyl Phthalate‐Induced Liver Tumors in Rodents

Journal of Applied Toxicology, EarlyView.
ABSTRACT Diisononyl phthalate (DINP) is a high molecular weight phthalate and high production volume chemical. DINP's carcinogenic potential has been investigated in four rodent bioassays, with liver tumors observed in three of the studies. Authoritative assessments have hypothesized that DINP acts through the peroxisome proliferator‐activated receptor
Amanda N. Buerger, Melissa M. Heintz, Laurie C. Haws, Chad M. Thompson   +3 more
wiley   +1 more source