Regulation of nuclear receptors PXR and CAR by small molecules and signal crosstalk: roles in drug metabolism and beyond

S Poudel, AD Huber, T Chen - Drug Metabolism and Disposition, 2023 - ASPET
Pregnane X receptor (PXR) and constitutive androstane receptor (CAR) are ligand-activated
transcription factors that regulate the expression of drug metabolizing enzymes and drug …

P450-humanized and human liver chimeric mouse models for studying xenobiotic metabolism and toxicity

KD Bissig, W Han, M Barzi, N Kovalchuk, L Ding… - Drug Metabolism and …, 2018 - ASPET
Preclinical evaluation of drug candidates in experimental animal models is an essential step
in drug development. Humanized mouse models have emerged as a promising alternative …

Highly sensitive electrochemical sensor for anticancer drug by a zirconia nanoparticle-decorated reduced graphene oxide nanocomposite

M Venu, S Venkateswarlu, YVM Reddy… - ACS …, 2018 - ACS Publications
Because of their large surface area and conductivity, some inorganic materials have
emerged as good candidates for the trace-level detection of pharmaceutical drugs. In the …

Designing out PXR activity on drug discovery projects: a review of structure-based methods, empirical and computational approaches

A Hall, H Chanteux, K Ménochet… - Journal of Medicinal …, 2021 - ACS Publications
This perspective discusses the role of pregnane xenobiotic receptor (PXR) in drug discovery
and the impact of its activation on CYP3A4 induction. The use of structural biology to reduce …

Identifying the reactive metabolites of tyrosine kinase inhibitors in a comprehensive approach: Implications for drug‐drug interactions and hepatotoxicity

MN Paludetto, F Puisset, E Chatelut… - Medicinal research …, 2019 - Wiley Online Library
Tyrosine kinase inhibitors (TKI) are small heterocyclic molecules targeting transmembrane
and cytoplasmic tyrosine kinases that have met with considerable success in clinical …

Functional Characterization of 22 CYP3A4 Protein Variants to Metabolize Ibrutinib In Vitro

R Xu, J Wen, P Tang, C Wang, S Xie… - Basic & Clinical …, 2018 - Wiley Online Library
Abstract Cytochrome P450 3A4 (CYP 3A4) is quantitatively the most important P450 enzyme
in adults. It is suggested that CYP 3A4 genetic polymorphisms may influence the rate of the …

Itraconazole-induced increases in gilteritinib exposure are mediated by CYP3A and OATP1B

DA Garrison, Y Jin, Z Talebi, S Hu, A Sparreboom… - Molecules, 2022 - mdpi.com
Gilteritinib, an FDA-approved tyrosine kinase inhibitor approved for the treatment of
relapsed/refractory FLT3-mutated acute myeloid leukemia, is primarily eliminated via …

[HTML][HTML] Chromatographic bioanalytical assays for targeted covalent kinase inhibitors and their metabolites

IA Retmana, JH Beijnen, RW Sparidans - Journal of Chromatography B, 2021 - Elsevier
Deriving from targeted kinase inhibitors (TKIs), targeted covalent kinase inhibitors (TCKIs)
are a new class of TKIs that are covalently bound to their target residue of kinase receptors …

Chaihu‐Shugan‐San Reinforces CYP3A4 Expression via Pregnane X Receptor in Depressive Treatment of Liver‐Qi Stagnation Syndrome

Z He, R Fan, C Zhang, T Tang, X Liu… - Evidence‐Based …, 2019 - Wiley Online Library
Backgrounds. Chaihu‐Shugan‐San (CSS) is a classic traditional Chinese herbal
prescription for treating depression. However, the underlying mechanism of the Chinese …

Metabolic bioactivation of antidepressants: advance and underlying hepatotoxicity

SM Khalil, KR MacKenzie… - Drug Metabolism …, 2024 - Taylor & Francis
Many drugs that serve as first-line medications for the treatment of depression are
associated with severe side effects, including liver injury. Of the 34 antidepressants …