In vitro safety signals for potential clinical development of the anti-inflammatory pregnane X receptor agonist FKK6

Z Dvořák, B Vyhlídalová, P Pečinková, H Li… - Bioorganic …, 2024 - Elsevier
Based on the mimicry of microbial metabolites, functionalized indoles were demonstrated as
the ligands and agonists of the pregnane X receptor (PXR). The lead indole, FKK6 …

Targeting the pregnane X receptor using microbial metabolite mimicry

Z Dvořák, F Kopp, CM Costello, JS Kemp… - EMBO molecular …, 2020 - embopress.org
The human PXR (pregnane X receptor), a master regulator of drug metabolism, has
essential roles in intestinal homeostasis and abrogating inflammation. Existing PXR ligands …

Deciphering structural bases of intestinal and hepatic selectivity in targeting pregnane X receptor with indole-based microbial mimics

H Li, P Illés, CV Karunaratne, LU Nordstrøm, X Luo… - Bioorganic …, 2021 - Elsevier
Microbial metabolite mimicry is a new concept that promises to deliver compounds that have
minimal liabilities and enhanced therapeutic effects in a host. In a previous publication, we …

Building a chemical toolbox for human pregnane X receptor research: discovery of agonists, inverse agonists, and antagonists among analogs based on the unique …

Y Li, W Lin, WC Wright, SC Chai, J Wu… - Journal of medicinal …, 2021 - ACS Publications
Pregnane X receptor (PXR) plays roles in detoxification and other physiological processes.
PXR activation may enhance drug metabolism (leading to adverse drug reactions) or inhibit …

[HTML][HTML] Characterization of human pregnane X receptor activators identified from a screening of the Tox21 compound library

C Lynch, S Sakamuru, R Huang, J Niebler… - Biochemical …, 2021 - Elsevier
The pregnane X receptor (PXR; NR1I2) is an important nuclear receptor whose main
function is to regulate enzymes within drug metabolism. The main drug metabolizing …

An evaluation of the anti-inflammatory properties of the pregnane X receptor gene isoforms PXR1 and PXR3

J Alleyne - European Journal of Inflammation, 2019 - journals.sagepub.com
The pregnane X receptor (PXR) is a nuclear receptor (NR) that primarily activates genes
involved in drug metabolism. However, PXR also suppresses inflammation. This study …

Total synthesis and pharmacological characterization of solomonsterol A, a potent marine pregnane-X-receptor agonist endowed with anti-inflammatory activity

V Sepe, R Ummarino, MV D'Auria… - Journal of medicinal …, 2011 - ACS Publications
Recently, we reported the identification of a novel class of pregnane-X-receptor (PXR)
agonists, solomonsterols A and B, isolated from the marine sponge Theonella swinhoei …

Pregnane X receptor and the gut-liver axis: a recent update

M Dutta, JJ Lim, JY Cui - Drug Metabolism and Disposition, 2022 - ASPET
It is well-known that the pregnane X receptor (PXR)/Nr1i2 is a critical xenobiotic-sensing
nuclear receptor enriched in liver and intestine and is responsible for drug-drug interactions …

Pregnane X receptor activation attenuates inflammation-associated intestinal epithelial barrier dysfunction by inhibiting cytokine-induced myosin light-chain kinase …

A Garg, A Zhao, SL Erickson, S Mukherjee… - … of Pharmacology and …, 2016 - ASPET
The inflammatory bowel diseases (IBDs) are chronic inflammatory disorders with a complex
etiology. IBD is thought to arise in genetically susceptible individuals in the context of …

Pregnane X receptor agonists enhance intestinal epithelial wound healing and repair of the intestinal barrier following the induction of experimental colitis

J Terc, A Hansen, L Alston, SA Hirota - European journal of pharmaceutical …, 2014 - Elsevier
The intestinal epithelial barrier plays a key role in the maintenance of homeostasis within the
gastrointestinal tract. Barrier dysfunction leading to increased epithelial permeability is …