Results 11 to 20 of about 235,181 (316)

The role of pregnane X receptor (PXR) in substance metabolism. [PDF]

Front Endocrinol (Lausanne), 2022
As a member of the nuclear receptor (NR) superfamily, pregnane X receptor (PXR; NR1I2) is a ligand-activated transcription factor that plays a crucial role in the metabolism of xenobiotics and endobiotics in mammals. The tissue distribution of PXR is parallel to its function with high expression in the liver and small intestine and moderate expression ...
Lv Y, Luo YY, Ren HW, Li CJ, Xiang ZX, Luan ZL.   +5 more
europepmc   +6 more sources

Pregnane X Receptor (PXR) Polymorphisms and Cancer Treatment. [PDF]

Biomolecules, 2021
Pregnane X Receptor (PXR) belongs to the nuclear receptors’ superfamily and mainly functions as a xenobiotic sensor activated by a variety of ligands. PXR is widely expressed in normal and malignant tissues. Drug metabolizing enzymes and transporters are also under PXR’s regulation. Antineoplastic agents are of particular interest since cancer patients
Skandalaki A, Sarantis P, Theocharis S.
europepmc   +8 more sources

SPA70 is a potent antagonist of human pregnane X receptor [PDF]

Nature Communications, 2017
AbstractMany drugs bind to and activate human pregnane X receptor (hPXR) to upregulate drug-metabolizing enzymes, resulting in decreased drug efficacy and increased resistance. This suggests that hPXR antagonists have therapeutic value. Here we report that SPA70 is a potent and selective hPXR antagonist.
Wenwei Lin, Yue-Ming Wang, Sergio C. Chai, Lili Lv, Jie Zheng, Jing Wu, Qijun Zhang, Yong-Dong Wang, Patrick R. Griffin, Taosheng Chen   +9 more
doaj   +5 more sources

Marine Ligands of the Pregnane X Receptor (PXR): An Overview [PDF]

Marine Drugs, 2019
Pregnane X Receptor (PXR) is a ligand-activated transcription factor which binds many structurally different molecules. The receptor is able to regulate the expression of a wide array of genes and is involved in cancer and different key physiological processes such as the metabolism of drugs/xenobiotics and endogenous compounds including lipids and ...
Alejandro Carazo, Přemysl Mladěnka, Petr Pávek   +2 more
doaj   +6 more sources

The constitutive androstane receptor and pregnane X receptor in the brain [PDF]

British Journal of Pharmacology, 2020
Since their discovery, the orphan nuclear receptors constitutive androstane receptor (CAR;NR1I3) and pregnane X receptor (PXR;NR1I2) have been regarded as master regulators of drug disposition and detoxification mechanisms. They regulate the metabolism and transport of endogenous mediators and xenobiotics in organs including the liver, intestine and ...
Francisca Espinoza, Jeffrey Penny, Pablo Torres-Vergara, Pablo Torres-Vergara, Carlos Escudero, Yu Siong Ho, Francisco Nualart   +6 more
openaire   +4 more sources

Evolution of pharmacologic specificity in the pregnane X receptor [PDF]

BMC Evolutionary Biology, 2008
Abstract Background The pregnane X receptor (PXR) shows the highest degree of cross-species sequence diversity of any of the vertebrate nuclear hormone receptors. In this study, we determined the pharmacophores for activation of human, mouse, rat, rabbit, chicken, and zebrafish PXRs, using a common set of sixteen ...
Sean Ekins, Sean Ekins, Lee R. Hagey, Matthew D. Krasowski, Erica J. Reschly   +4 more
openaire   +5 more sources

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   +2 more sources

Functional evolution of the pregnane X receptor [PDF]

Expert Opinion on Drug Metabolism & Toxicology, 2006
The pregnane X receptor (PXR; NR1I2) is a nuclear hormone receptor (NR) that transcriptionally regulates genes encoding transporters and drug-metabolising enzymes in the liver and intestine. PXR activation leads to enhanced metabolism and elimination of xenobiotics and endogenous compounds such as hormones and bile salts.
Erica J. Reschly, Manisha Iyer, Matthew D. Krasowski   +2 more
openaire   +4 more sources

Cholesterol detoxification by the nuclear pregnane X receptor [PDF]

Proceedings of the National Academy of Sciences, 2005
We have a love–hate relationship with cholesterol. On one hand, cholesterol is an essential component of cell membranes and serves as the precursor to steroid hormones and bile acids. On the other hand, cholesterol can clog blood vessels and give rise to cardiovascular disease.
Steven A. Kliewer
openaire   +5 more sources

Associations between Pregnane X Receptor and Breast Cancer Growth and Progression. [PDF]

Cells, 2020
Pregnane X receptor (PXR, NR1I2) is a member of the ligand-activated nuclear receptor superfamily. This receptor is promiscuous in its activation profile and is responsive to a broad array of both endobiotic and xenobiotic ligands.
Creamer BA, Sloan SNB, Dennis JF, Rogers R, Spencer S, McCuen A, Persaud P, Staudinger JL.   +7 more
europepmc   +3 more sources