Results 51 to 60 of about 43,637 (267)
British Journal of Clinical Pharmacology, EarlyView.While the event‐free survival (EFS) of children treated for acute lymphoblastic leukaemia (ALL) has improved greatly in the last decades, the EFS for patients diagnosed with ALL before the age of one is still under 50%. This outcome further decreases when infants have a rearrangement in the gene encoding histone‐lysine N‐methyltransferase 2A (KMT2A ...
Tirsa de Kluis +5 more
wiley +1 more source
Anion-Dependent Stimulation of CYP3A4 Monooxygenase [PDF]
Biochemistry, 2015 We co-crystallized human cytochrome P450 3A4 (CYP3A4) with progesterone (PRG) under two different conditions, but the resulting complexes contained only one PRG molecule bound to the previously identified peripheral site. A novel feature in one of our structures is a citrate ion, originating from the crystallization solution.
Sevrioukova, Irina F, Poulos, Thomas L
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Precision medicine in paediatrics: Progress and priorities
British Journal of Clinical Pharmacology, EarlyView.Precision medicine is revolutionizing personalized healthcare, advancing both diagnostics and therapeutics at an unprecedented pace. Reviewing the paediatric applications of pharmacometrics, pharmacogenomics and advanced therapy medicinal products highlights not only the relevance of these exciting innovations to frontline care but also the significant
Nicola Husain +3 more
wiley +1 more source
British Journal of Clinical Pharmacology, EarlyView.Abstract Aim Sirolimus is currently used off‐label for paediatric patients with vascular anomalies. However, the optimal dosage regimen for paediatric patients remains controversial. This study aimed to determine the optimal dosing regimen of sirolimus in these patients using a population pharmacokinetic (PK) model.
Seongmee Jeong +13 more
wiley +1 more source
Transcriptional Regulation and Expression of CYP3A4 in Hepatocytes
Current Drug Metabolism, 2007 CYP3A4 is the most abundantly expressed drug-metabolizing P450 enzyme in human liver and contributes to the metabolism of a large number of drugs in use today. CYP3A4 is constitutively expressed in adult hepatocytes but it can also be transcriptionally induced by a variety of structurally diverse xenochemicals.
Martinez Jimenez, Celia Pilar +4 more
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British Journal of Clinical Pharmacology, EarlyView.Aim The number of pregnancies among women with cystic fibrosis (wwCF) has steadily increased over the past decade. However, the pharmacokinetics (PK) of elexacaftor–tezacaftor–ivacaftor (ETI) during gestation remains uncharacterized, despite its widespread use in this population.
Paulette Magnas +16 more
wiley +1 more source
Induced fit for cytochrome P450 3A4 based on molecular dynamics
ADMET and DMPK, 2019 The present study aims at numerically describing to what extent substrate - enzyme complexes in solution may change over time as a natural process of conformational changes for a liganded enzyme in comparison to those movements which occur independently ...
Thomas R.F. Scior, Israel Quiroga
doaj +1 more source
Inhibition of CYP3A4 by 6′,7′-dihydroxybergamottin in human CYP3A4 over-expressed hepG2 cells
Journal of Pharmacy and Pharmacology, 2012 AbstractObjectivesWe previously established HepG2-GS-3A4, a cell line from hepatoblastoma with overexpression of human CYP3A4 and glutamine synthetase (GS). We further reported that these cells can be applied for screening inhibitors of CYP3A4 in vitro.
Nobutaka, Araki +7 more
openaire +2 more sources
Pharmacokinetic profiling of imatinib in relation to CYP3A4 activity in leukaemia patients
British Journal of Clinical Pharmacology, EarlyView.Aim Imatinib pharmacokinetics exhibit large interindividual variability because of differences in CYP3A4 activity—the main imatinib‐metabolizing enzyme. While therapeutic drug monitoring is effective, it requires steady‐state conditions and frequent sampling.
Anna Sofie Buhl Rasmussen +14 more
wiley +1 more source
British Journal of Clinical Pharmacology, EarlyView.Aims CYP2C19 is one of the most important pharmacogenes, and its activity is highly variable due to factors such as genetics or drug–drug interactions. Due to the lack of an appropriate endogenous CYP2C19 biomarker, surrogate methods to assess its activity are warranted.
Julian Peter Müller +9 more
wiley +1 more source