Results 1 to 10 of about 756 (108)

PXR and 4β-Hydroxycholesterol Axis and the Components of Metabolic Syndrome [PDF]

open access: yesCells, 2020
Pregnane X receptor (PXR) activation has been found to regulate glucose and lipid metabolism and affect obesity in response to high-fat diets. PXR also modulates vascular tone.
Janne Hukkanen, Jukka Hakkola
doaj   +5 more sources

Role of oxysterol 4β-hydroxycholesterol and liver X receptor alleles in pre-eclampsia [PDF]

open access: yesAnnals of Medicine
Background Liver X receptors (LXRs) are expressed in placenta and may be associated with pre-eclampsia (PE). Oxysterols act as agonists for LXRs. We recently proposed a new blood pressure-regulating circuit with oxysterol 4β-hydroxycholesterol (4βHC ...
Lassi Kaartinen   +13 more
doaj   +5 more sources

Esterification of 4β-hydroxycholesterol and other oxysterols in human plasma occurs independently of LCAT [PDF]

open access: yesJournal of Lipid Research, 2020
The acyltransferase LCAT mediates FA esterification of plasma cholesterol. In vitro studies have shown that LCAT also FA-esterifies several oxysterols, but in vivo evidence is lacking. Here, we measured both free and FA-esterified forms of sterols in 206
Daisuke Yamamuro   +12 more
doaj   +5 more sources

Clinical Evaluation Based on a New Approach to Improve the Accuracy of 4β-Hydroxycholesterol Measurement as a Biomarker of CYP3A4 Activity [PDF]

open access: yesMolecules, 2023
This study examines 4β-Hydroxycholesterol (4β-HC), which is considered to be a potential marker for the CYP3A4 induction of new chemical entities (NCEs) in drug development.
Yuki Taya   +6 more
doaj   +2 more sources

4β-Hydroxycholesterol is a prolipogenic factor that promotes SREBP1c expression and activity through the liver X receptor [PDF]

open access: yesJournal of Lipid Research, 2021
Oxysterols are oxidized derivatives of cholesterol that play regulatory roles in lipid biosynthesis and homeostasis. How oxysterol signaling coordinates different lipid classes such as sterols and triglycerides remains incompletely understood.
Ofer Moldavski   +11 more
doaj   +2 more sources

Formation of CYP3A‐specific metabolites of ibrutinib in vitro is correlated with hepatic CYP3A activity and 4β‐hydroxycholesterol/cholesterol ratio [PDF]

open access: yesClinical and Translational Science, 2023
Ibrutinib is an orally administered Bruton's tyrosine kinase inhibitor approved for the treatment of B‐cell malignancies, including chronic lymphocytic leukemia.
Jonghwa Lee   +3 more
doaj   +2 more sources

Pregnane X Receptor‒4β‐Hydroxycholesterol Axis in the Regulation of Overweight‐ and Obesity‐Induced Hypertension [PDF]

open access: yesJournal of the American Heart Association: Cardiovascular and Cerebrovascular Disease, 2022
Background Mechanisms mediating hypertensive effects of overweight and obesity have not been fully elucidated. We showed previously that activation of pregnane X receptor (PXR) by rifampicin elevates 24‐hour blood pressure (BP) and plasma 4β ...
Roosa Rahunen   +6 more
doaj   +2 more sources

The utility of endogenous glycochenodeoxycholate-3-sulfate and 4β-hydroxycholesterol to evaluate the hepatic disposition of atorvastatin in rats [PDF]

open access: yesAsian Journal of Pharmaceutical Sciences, 2021
The liver is an important organ for drugs disposition, and thus how to accurately evaluate hepatic clearance is essential for proper drug dosing. However, there are many limitations in drug dosage adjustment based on liver function and pharmacogenomic ...
Yanrong Ma   +6 more
doaj   +2 more sources

Applications of the Cholesterol Metabolite, 4β-Hydroxycholesterol, as a Sensitive Endogenous Biomarker for Hepatic CYP3A Activity Evaluated within a PBPK Framework [PDF]

open access: yesPharmaceutics
Background/Objectives: Plasma levels of 4β-hydroxycholesterol (4β-OHC), a CYP3A-specific metabolite of cholesterol, are elevated after administration of CYP3A inducers like rifampicin and carbamazepine.
Aneesh V. Karkhanis   +4 more
doaj   +2 more sources

Evaluation of the usefulness of plasma 4β‐hydroxycholesterol concentration normalized by 4α‐hydroxycholesterol for accurate CYP3A phenotyping [PDF]

open access: yesClinical and Translational Science
Plasma 4β‐hydroxycholesterol (OHC) has drawn attention as an endogenous substrate indicating CYP3A activity. Plasma 4β‐OHC is produced by hydroxylation by CYP3A4 and CYP3A5 and by cholesterol autoxidation.
Ayako Oda   +14 more
doaj   +2 more sources

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