Perspective on quantitative structure–toxicity relationship (QSTR) models to predict hepatic biotransformation of xenobiotics

M Rai, N Paudel, M Sakhrie, D Gemmati, IA Khan… - Livers, 2023 - mdpi.com
Biotransformation refers to the metabolic conversion of endogenous and xenobiotic
chemicals into more hydrophilic substances. Xenobiotic biotransformation is accomplished …

Plasma protein-mediated uptake and contradictions to the free drug hypothesis: a critical review

JA Schulz, DM Stresser, JC Kalvass - Drug metabolism reviews, 2023 - Taylor & Francis
According to the free drug hypothesis (FDH), only free, unbound drug is available to interact
with biological targets. This hypothesis is the fundamental principle that continues to explain …

[HTML][HTML] Comparative analysis of YAP/TEAD inhibitors in 2D and 3D cultures of primary human hepatocytes reveals a novel non-canonical mechanism of CYP …

N Oliva-Vilarnau, SU Vorrink, FA Büttner… - Biochemical …, 2023 - Elsevier
Induction of cytochrome P450 (CYP) genes constitutes an important cause of drug–drug
interactions and preclinical evaluation of induction liability is mandatory for novel drug …

Drug metabolism of hepatocyte-like organoids and their applicability in in vitro toxicity testing

MC Bouwmeester, Y Tao, S Proença… - Molecules, 2023 - mdpi.com
Emerging advances in the field of in vitro toxicity testing attempt to meet the need for reliable
human-based safety assessment in drug development. Intrahepatic cholangiocyte …

Multi-well array culture of primary human hepatocyte spheroids for clearance extrapolation of slowly metabolized compounds

LC Preiss, VM Lauschke, K Georgi, C Petersson - The AAPS Journal, 2022 - Springer
Accurate prediction of human pharmacokinetics using in vitro tools is an important task
during drug development. Albeit, currently used in vitro systems for clearance extrapolation …

Oxidized Soybean Oil Evoked Hepatic Fatty Acid Metabolism Disturbance in Rats and their Offspring

F Gao, X Guan, W Zhang, T Han, X Liu… - Journal of Agricultural …, 2023 - ACS Publications
The oxidation of fats and oils is an undisputed subject of science, given the effect of oxidized
fats and oils on food quality and safety. This study aimed to determine whether maternal …

The therapeutic potential of natural metabolites in targeting endocrine-independent HER-2-negative breast cancer

M Püsküllüoğlu, I Michalak - Frontiers in Pharmacology, 2024 - frontiersin.org
Breast cancer (BC) is a heterogenous disease, with prognosis and treatment options
depending on Estrogen, Progesterone receptor, and Human Epidermal Growth Factor …

Multiplexed In Vivo Screening Using Barcoded Aptamer Technology to Identify Oligonucleotide-Based Targeting Reagents

BJ Thomas, C Guldenpfennig, MA Daniels… - nucleic acid …, 2024 - liebertpub.com
Recent FDA approvals of mRNA vaccines, short-interfering RNAs, and antisense
oligonucleotides highlight the success of oligonucleotides as therapeutics. Aptamers are …

Clinical insights on caloric restriction mimetics for mitigating brain aging and related neurodegeneration

A Trisal, AK Singh - Cellular and Molecular Neurobiology, 2024 - Springer
Aging, an inevitable physiological process leading to a progressive decline in bodily
functions, has been an abundantly researched domain with studies attempting to slow it …

The choice of ultra‐low attachment plates impacts primary human and primary canine hepatocyte spheroid formation, phenotypes, and function

C Xing, A Kemas, E Mickols, K Klein… - Biotechnology …, 2024 - Wiley Online Library
Organotypic three‐dimensional liver spheroid cultures in which hepatic cells retain their
molecular phenotype and functionality have emerged as powerful tools for preclinical drug …