Results 111 to 120 of about 16,921 (212)

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

The 3ʹ-untranslated region contributes to the pregnane X receptor (PXR) expression down-regulation by PXR ligands and up-regulation by glucocorticoids

Acta Pharmaceutica Sinica B, 2020
Pregnane X receptor (PXR) is the major regulator of xenobiotic metabolism. PXR itself is controlled by various signaling molecules including glucocorticoids. Moreover, negative feed-back regulation has been proposed at the transcriptional level.
Tomas Smutny, Jan Dusek, Lucie Hyrsova, Jana Nekvindova, Alzbeta Horvatova, Stanislav Micuda, Sabine Gerbal-Chaloin, Petr Pavek   +7 more
doaj   +1 more source

The Furan Fatty Acids 11M5 and 11D5 Can Act as Activators of Human Peroxisome Proliferator‐Activated Receptor Gamma

Molecular Nutrition &Food Research, Volume 69, Issue 24, December 2025.
Furan fatty acids are abundant in food such as fatty fish. Here we show that some of these can bind to and act as activators of the nuclear receptors, peroxisome proliferator‐activated receptor gamma (PPAR‐gamma) and retinoid X receptor (RXR), in human cells.
Jonas Pospiech, Ayelet Caspi, Walter Vetter, Zohar Kerem, Jan Frank, Thomas A. Kufer   +5 more
wiley   +1 more source

Rifampin modulation of xeno- and endobiotic conjugating enzyme mRNA expression and associated microRNAs in human hepatocytes [PDF]

, 2018
Rifampin is a pleiotropic inducer of multiple drug metabolizing enzymes and transporters. This work utilized a global approach to evaluate rifampin effects on conjugating enzyme gene expression with relevance to human xeno- and endo-biotic metabolism ...
Desta, Zeruesenay, Eadon, Michael T., Gao, Hongyu, Gufford, Brandon T., Lin, Hai, Liu, Yunlong, Robarge, Jason D., Skaar, Todd C.   +7 more
core   +1 more source

Characterization of porcine pregnane X receptor, farnesoid X receptor and their splice variants

Experimental Biology and Medicine, 2010
The pregnane X receptor (PXR; NR1I2) and the farnesoid X receptor (FXR; NR1H4) regulate the expression of many major metabolic enzymes. With the pig being used as a model for humans in metabolic and toxicological studies and also an important food animal, we characterized the transactivation profile of the porcine orthologs of these receptors, pgPXR ...
Matthew A, Gray, Callie B, Pollock, Lawrence B, Schook, E James, Squires   +3 more
openaire   +2 more sources

Phenobarbital-mediated tumor promotion in transgenic mice with humanized CAR and PXR [PDF]

, 2014
The nuclear receptors CAR (constitutive androstane receptor) and possibly PXR (pregnane X receptor) mediate the hepatic effects of phenobarbital (PB) and similar-acting compounds.
Braeuning, Albert, Brown, Susan, Gavrilov, Alina, Henderson, Colin J, Schwarz, Michael, Wolf, C Roland   +5 more
core   +2 more sources

Generation of a PXR reporter human induced pluripotent stem cell line (PXR-mCherry hiPSC) using the CRISPR/Cas9 system

Stem Cell Research, 2018
Pregnane X receptor (PXR) is a key nuclear receptor that mediates drug metabolism and stimulates hepatocyte proliferation. However, the lack of PXR expression in human pluripotent stem cell-derived hepatocytes limits their application for drug screening ...
Hyemin Kim, Ji-Woo Kim, So-Jin Kim, Young-Jun Choi, Dae-Sung Kim, Han-Jin Park   +5 more
doaj   +1 more source

Integration of Genome Scale Metabolic Networks and gene regulation of metabolic enzymes with Physiologically Based Pharmacokinetics [PDF]

, 2017
The scope of Physiologically Based Pharmacokinetic (PBPK) modelling can be expanded by assimilation of the mechanistic models of intracellular processes from Systems Biology field.
Al Olama, Alimirah, Arshad, Ay, Bailey, Beste, Blätke, Bordbar, Cannon, Covert, Covert, El-Sankary, Fell, Fisher, Giacomantonio, Gibson, Gille, Goss, Guebila, Heino, Huang, Huang, Huizenga, Jain, Jin, Jones, Kobayashi, Kolodkin, Kotas, Krauss, Lee, Lewis, Mark, Matsuno, Murata, Oakley, Orth, Pascussi, Plant, Reul, Schellenberger, Schilling, Schuster, Shmulevich, Steggles, Stephanopoulos, Varma, Watkins, Wienkers, Wu, Xiao, Zhang   +51 more
core   +2 more sources

High Definition Immunoassays (HDIA) with Spatially Resolved Detection [PDF]

, 2012
Dealing with problem-solving has been a growing challenge in teaching engineering and over the career of these professionals. To increase the ability to understand a problem and consequently improve the quality of the solutions, an exercise was proposed ...
Ruan, Qiaoqiao, Skinner, Joseph P., Tetin, Sergey Y.   +2 more
core   +4 more sources

The phenolic complex in flaxseed [PDF]

, 2008
Flaxseed is the richest plant source of the lignan secoisolariciresinol diglucoside (SDG). In flaxseed, SDG exists in an oligomeric structure with 3-hydroxy-3-methyl glutaric acid (HMGA) forming a phenolic complex together with p-coumaric acid and ...
Strandås, Christina
core