Results 1 to 10 of about 775 (125)

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

Cells, 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

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

Journal 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, Hisataka Yamazaki, Jun-ichi Osuga, Kenta Okada, Tetsuji Wakabayashi, Akihito Takei, Shoko Takei, Manabu Takahashi, Shuichi Nagashima, Adriaan G. Holleboom, Masayuki Kuroda, Hideaki Bujo, Shun Ishibashi   +12 more
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Clinical Evaluation Based on a New Approach to Improve the Accuracy of 4β-Hydroxycholesterol Measurement as a Biomarker of CYP3A4 Activity [PDF]

Molecules, 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, Mari Mizunaga, Shunsuke Nakao, Mirinthorn Jutanom, Naoki Shimizu, Yukihiro Nomura, Kiyotaka Nakagawa   +6 more
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4β-Hydroxycholesterol is a prolipogenic factor that promotes SREBP1c expression and activity through the liver X receptor [PDF]

Journal 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, Peter-James H. Zushin, Charles A. Berdan, Robert J. Van Eijkeren, Xuntian Jiang, Mingxing Qian, Daniel S. Ory, Douglas F. Covey, Daniel K. Nomura, Andreas Stahl, Ethan J. Weiss, Roberto Zoncu   +11 more
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Formation of CYP3A‐specific metabolites of ibrutinib in vitro is correlated with hepatic CYP3A activity and 4β‐hydroxycholesterol/cholesterol ratio [PDF]

Clinical 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, John K. Fallon, Philip C. Smith, Klarissa D. Jackson   +3 more
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Pregnane X Receptor‒4β‐Hydroxycholesterol Axis in the Regulation of Overweight‐ and Obesity‐Induced Hypertension [PDF]

Journal 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, Outi Kummu, Vesa Koivukangas, Heidi Hautajärvi, Jukka Hakkola, Jaana Rysä, Janne Hukkanen   +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]

Asian 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, Mingyan Xin, Yuanjie Wen, Huan Wang, Guoqiang Zhang, Jianye Dai, Xin-An Wu   +6 more
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Applications of the Cholesterol Metabolite, 4β-Hydroxycholesterol, as a Sensitive Endogenous Biomarker for Hepatic CYP3A Activity Evaluated within a PBPK Framework [PDF]

Pharmaceutics
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, Matthew D. Harwood, Felix Stader, Frederic Y. Bois, Sibylle Neuhoff   +4 more
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Evaluation of the usefulness of plasma 4β‐hydroxycholesterol concentration normalized by 4α‐hydroxycholesterol for accurate CYP3A phenotyping [PDF]

Clinical 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, Yosuke Suzuki, Haruki Sato, Teruhide Koyama, Masahiro Nakatochi, Yukihide Momozawa, Ryota Tanaka, Hiroyuki Ono, Ryosuke Tatsuta, Tadasuke Ando, Toshitaka Shin, Kenji Wakai, Keitaro Matsuo, Hiroki Itoh, Keiko Ohno   +14 more
doaj   +2 more sources

4β-Hydroxycholesterol Signals From the Liver to Regulate Peripheral Cholesterol Transporters [PDF]

Frontiers in Pharmacology, 2020
Activation of pregnane X receptor (PXR) elevates circulating 4β-hydroxycholesterol (4βHC), an agonist of liver X receptor (LXR). PXR may also regulate 25-hydroxycholesterol and 27-hydroxycholesterol.
Tuire Salonurmi, Tuire Salonurmi, Heba Nabil, Heba Nabil, Heba Nabil, Justiina Ronkainen, Justiina Ronkainen, Tuulia Hyötyläinen, Heidi Hautajärvi, Markku J. Savolainen, Markku J. Savolainen, Markku J. Savolainen, Ari Tolonen, Matej Orešič, Päivi Känsäkoski, Jaana Rysä, Jukka Hakkola, Jukka Hakkola, Jukka Hakkola, Janne Hukkanen, Janne Hukkanen, Janne Hukkanen   +21 more
doaj   +2 more sources