Quantitative analysis of 4β- and 4α‑hydroxycholesterol in human plasma and serum by UHPLC/ESI-HR-MS [PDF]
, 2020 Cholesterol oxidation product 4β‑hydroxycholesterol (4β‑OHC) may possibly be used as an endogenous biomarker of CYP3A enzyme activity and as CYP3A4 is involved in the metabolism of approximately 50% of the drugs in clinical use, the monitoring of CYP3A ...
Hautajärvi, Heidi +4 more
core +1 more source
Rifampicin induces the bone form of alkaline phosphatase in humans [PDF]
, 2021 Pregnane X receptor (PXR) is a xenobiotic-sensing nuclear receptor that regulates drug metabolism in the liver and intestine. In our clinical trials on healthy volunteers to discover novel metabolic functions of PXR activation, we observed that ...
Hakkola, Jukka +6 more
core +1 more source
Impact of CYP3A5 genotype on tolvaptan pharmacokinetics and their relationships with endogenous markers of CYP3A activity and serum sodium level in heart failure patients [PDF]
, 2020 Tolvaptan efficacy for heart failure has a large interindividual variation. This study aimed to evaluate the influence of CYP3A5 and ABCB1 genotypes on tolvaptan pharmacokinetics and their relationships with plasma markers of CYP3A activity and ...
Akutsu, Shunta +5 more
core +1 more source
The 1β-Hydroxy-Deoxycholic Acid to Deoxycholic Acid Urinary Metabolic Ratio: Toward a Phenotyping of CYP3A Using an Endogenous Marker? [PDF]
, 2021 In this study, we assessed the potential use of the 1β-hydroxy-deoxycholic acid (1β-OH-DCA) to deoxycholic acid (DCA) urinary metabolic ratio (UMR) as a CYP3A metric in ten male healthy volunteers.
Bosilkovska, M. +4 more
core +2 more sources
Clinical and Translational Science, 2022 Bintrafusp alfa, a first‐in‐class bifunctional fusion protein composed of the extracellular domain of TGF‐βRII (a TGF‐β “trap”) fused to a human IgG1 mAb blocking PD‐L1, is being evaluated for efficacy and safety in solid tumor indications as monotherapy
Yulia Vugmeyster +5 more
doaj +1 more source
Besnoitia besnoiti infection alters both endogenous cholesterol de novo synthesis and exogenous LDL uptake in host endothelial cells [PDF]
, 2008 Besnoitia besnoiti, an apicomplexan parasite of cattle being considered as emergent in Europe, replicates fast in host endothelial cells during acute infection and is in considerable need for energy, lipids and other building blocks for offspring ...
Silva, Liliana M. R. +8 more
core +2 more sources
Journal of Lipid Research, 2002 Oxysterols possess powerful biological activities. Some of their effects on the regulation of key enzymes are similar to those of cholesterol, but are much more potent.
Steve Meaney +3 more
doaj +1 more source
Comparison of the Pharmacokinetics of RIPK1 Inhibitor GSK2982772 in Healthy Western and Japanese Subjects. [PDF]
, 2021 Funder: GlaxoSmithKline; doi: http://dx.doi.org/10.13039/100004330BACKGROUND AND OBJECTIVES: GSK2982772 is an oral small-molecule RIPK1 inhibitor with potential therapeutic efficacy in immune-mediated inflammatory diseases (IMIDs).
Cannons, Edward P +12 more
core +1 more source
Cholesterol 25-hydroxylation activity of CYP3A
Journal of Lipid Research, 2011 To date, many studies have been conducted using 25-hydroxycholesterol, which is a potent regulator of lipid metabolism. However, the origins of this oxysterol have not been entirely elucidated. Cholesterol 25-hydroxylase is one of the enzymes responsible
Akira Honda +8 more
doaj +1 more source
Deconvoluting Gut Versus Liver Cytochrome P450 3A4 Function: Drug Probes, Biomarkers, and Tissue Biopsy. [PDF]
J Clin PharmacolAbstract Cytochrome P450 3A4 (CYP3A4) is an important drug‐metabolizing enzyme, whose function is impacted by age, sex, body weight, pregnancy, and disease. It is also the site of major drug interactions involving inhibition and induction. Because CYP3A4 is expressed in the intestine and liver, investigators have sought to study its function in both ...
Rodrigues D.
europepmc +2 more sources