Effect of Individual and Combined Cytochrome P450 Activity Scores on Symptom Improvement and Side Effects in Youth Treated With Sertraline. [PDF]
Gerlach S +7 more
europepmc +1 more source
Introduction to Single‐Cell Physiologically‐Based Pharmacokinetic (scPBPK) Models
ABSTRACT The current investigation introduces single‐cell physiologically based pharmacokinetic (scPBPK) models to gain insight into drug disposition at the cellular scale. The transition from standard PBPK (sPBPK) models to scPBPK models required depiction of expression‐dependent (ED) processes, such as drug metabolism or membrane transport.
Anshul Saini, James M. Gallo
wiley +1 more source
Mineralocorticoid Receptor Antagonists in Chronic Kidney Disease: Clinical Evidence, Pharmacology, and Drug-Drug Interactions for Personalized Management of Hyperkalemia. [PDF]
Hirai T, Katayama K.
europepmc +1 more source
ABSTRACT Background and Aims Metabolic dysfunction‐associated steatotic liver disease (MASLD) is a progressive liver disease that ranges from simple steatosis to inflammation, fibrosis and cirrhosis. To address the unmet need for new MASLD biomarkers, we aimed to identify candidate biomarkers using publicly available RNA sequencing (RNA‐seq) and ...
Wenfeng Ma +17 more
wiley +1 more source
The impact of NK1 receptor antagonist selection on chemotherapy-related adverse events: a retrospective study of adverse events in paclitaxel or nab-paclitaxel and carboplatin combination therapy with fosnetupitant and aprepitant use. [PDF]
Yamaoka K +7 more
europepmc +1 more source
From Fragments to Function: Novel Hydrazone Derivatives as Monoamine Oxidase Inhibitors
Twelve N‐acylhydrazone derivatives (5a–f, 6a–f) were synthesized and characterized. Compounds displayed potent submicromolar inhibition against both MAO‐A and MAO‐B. Compound 6e exhibited the strongest activity (IC50 = 0.073 μM for MAO‐A; 0.064 μM for MAO‐B). Kinetic and docking analyses confirmed reversible, competitive inhibition via FAD interaction.
Hasan Erdinç Sellitepe +5 more
wiley +1 more source
Deconvoluting Gut Versus Liver Cytochrome P450 3A4 Function: Drug Probes, Biomarkers, and Tissue Biopsy. [PDF]
Rodrigues D.
europepmc +1 more source
Can an amide analog retain the high potency of the classic urea motif in soluble epoxide hydrolase inhibitors? Through a single unconventional switch, the introduction of the underexplored pentafluorosulfanyl group into an amide analog of TPPU, the authors restored high inhibitory potency.
Alba López‐Ruiz +17 more
wiley +1 more source
Development of an Empirical Approach for the Prediction of Cytochrome P450-Based Drug-Drug Interactions in Pediatric Patients. [PDF]
Di Paolo V +3 more
europepmc +1 more source
A novel pyridine–thiazole derivative, Compound 8, exhibited potent dual antitrypanosomatid activity. It demonstrated remarkable in vitro efficacy against Trypanosoma cruzi (IC50 = 1.0 µM) and L. amazonensis (IC50 = 3.9 µM). Molecular docking studies suggested interactions with heme and multiple molecular targets.
Anderson José Firmino Santos da Silva +10 more
wiley +1 more source

