Mechanisms of xenobiotic receptor activation: Direct vs. indirect

B Mackowiak, H Wang - Biochimica et Biophysica Acta (BBA)-Gene …, 2016 - Elsevier
The so-called xenobiotic receptors (XRs) have functionally evolved into cellular sensors for
both endogenous and exogenous stimuli by regulating the transcription of genes encoding …

Reporter cell lines for the characterization of the interactions between human nuclear receptors and endocrine disruptors

M Grimaldi, A Boulahtouf, V Delfosse… - Frontiers in …, 2015 - frontiersin.org
Endocrine-disrupting chemicals (EDCs) are exogenous substances interfering with hormone
biosynthesis, metabolism, or action, and consequently causing disturbances in the …

Evaluating wear volume of oligoether esters with an interpretable machine learning approach

H Wang, C Zhang, X Yu, Y Li - Tribology Letters, 2023 - Springer
Wear is a familiar tribological failure in liquid lubrication, especially for low-viscosity base
oils without any additives. Therefore, it is necessary to understand and evaluate the anti …

Fish as a model to assess chemical toxicity in bone

I Fernández, PJ Gavaia, V Laize, ML Cancela - Aquatic Toxicology, 2018 - Elsevier
Environmental toxicology has been expanding as growing concerns on the impact of
produced and released chemical compounds over the environment and human health are …

P2Y1 purinergic receptor identified as a diabetes target in a small-molecule screen to reverse circadian β-cell failure

B Marcheva, BJ Weidemann, A Taguchi, M Perelis… - Elife, 2022 - elifesciences.org
The mammalian circadian clock drives daily oscillations in physiology and behavior through
an autoregulatory transcription feedback loop present in central and peripheral cells …

Review of in silico studies dedicated to the nuclear receptor family: Therapeutic prospects and toxicological concerns

A Sellami, M Réau, M Montes, N Lagarde - Frontiers in Endocrinology, 2022 - frontiersin.org
Being in the center of both therapeutic and toxicological concerns, NRs are widely studied
for drug discovery application but also to unravel the potential toxicity of environmental …

Regulation of pxr function by coactivator and corepressor proteins: Ligand binding is just the beginning

JP Rigalli, D Theile, J Nilles, J Weiss - Cells, 2021 - mdpi.com
The pregnane X receptor (PXR, NR1I2) is a nuclear receptor which exerts its regulatory
function by heterodimerization with the retinoid-X-receptor α (RXRα, NR2B1) and binding to …

Chemical screening of nuclear receptor modulators

M Ishigami-Yuasa, H Kagechika - International journal of molecular …, 2020 - mdpi.com
Nuclear receptors are ligand-inducible transcriptional factors that control multiple biological
phenomena, including proliferation, differentiation, reproduction, metabolism, and the …

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 …

Identification of approved drugs as potent inhibitors of pregnane X receptor activation with differential receptor interaction profiles

O Burk, M Kuzikov, T Kronenberger, J Jeske… - Archives of …, 2018 - Springer
Activation of pregnane X receptor (PXR) results in the induction of first-pass metabolism and
drug efflux. Hereby, PXR may cause adverse drug reactions or therapeutic failure of drugs …