University of Oulu

Karpale, M., Hukkanen, J., & Hakkola, J. (2022). Nuclear Receptor PXR in Drug-Induced Hypercholesterolemia. Cells, 11(3), 313.

Nuclear receptor PXR in drug-induced hypercholesterolemia

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Author: Karpale, Mikko1; Hukkanen, Janne2; Hakkola, Jukka1
Organizations: 1Research Unit of Biomedicine, Biocenter Oulu, Medical Research Center Oulu, University of Oulu and Oulu University Hospital, P.O. Box 5000, FI-90014 Oulu, Finland
2Research Unit of Internal Medicine, Biocenter Oulu, Medical Research Center Oulu, University of Oulu and Oulu University Hospital, P.O. Box 5000, FI-90014 Oulu, Finland
Format: article
Version: published version
Access: open
Online Access: PDF Full Text (PDF, 0.8 MB)
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Language: English
Published: Multidisciplinary Digital Publishing Institute, 2022
Publish Date: 2022-05-17


Atherosclerosis is a major global health concern. The central modifiable risk factors and causative agents of the disease are high total and low-density lipoprotein (LDL) cholesterol. To reduce morbidity and mortality, a thorough understanding of the factors that influence an individual’s cholesterol status during the decades when the arteria-narrowing arteriosclerotic plaques are forming is critical. Several drugs are known to increase cholesterol levels; however, the mechanisms are poorly understood. Activation of pregnane X receptor (PXR), the major regulator of drug metabolism and molecular mediator of clinically significant drug–drug interactions, has been shown to induce hypercholesterolemia. As a major sensor of the chemical environment, PXR may in part mediate hypercholesterolemic effects of drug treatment. This review compiles the current knowledge of PXR in cholesterol homeostasis and discusses the role of PXR in drug-induced hypercholesterolemia.

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Series: Cells
ISSN: 2073-4409
ISSN-E: 2073-4409
ISSN-L: 2073-4409
Volume: 11
Issue: 3
Article number: 313
DOI: 10.3390/cells11030313
Type of Publication: A2 Review article in a scientific journal
Field of Science: 3121 General medicine, internal medicine and other clinical medicine
3111 Biomedicine
Funding: The original research of the authors has been financially supported by the grants from the Academy of Finland (grants 286743 and 323706), the Novo Nordisk Foundation (grants NNF14OC0010653 and NNF15OC0015846), the Finnish Medical Foundation, the Finnish Foundation for Cardiovascular Research, the Northern Finland Health Care Support Foundation, and the Diabetes Research Foundation. The project EDCMET has received funding from the European Union’s Horizon 2020 research and innovation programme under grant agreement no. 825762.
EU Grant Number: (825762) EDCMET - Metabolic effects of Endocrine Disrupting Chemicals: novel testing METhods and adverse outcome pathways
Academy of Finland Grant Number: 286743
Detailed Information: 286743 (Academy of Finland Funding decision)
323706 (Academy of Finland Funding decision)
Copyright information: © 2022 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (