Liver X receptors in lipid metabolism: opportunities for drug discovery
Abstract
The liver X receptors (LXRs) are pivotal regulators of lipid homeostasis in mammals. These transcription factors control the expression of a battery of genes involved in the uptake, transport, efflux and excretion of cholesterol in a tissue-dependent manner. The identification of the LXRs, and an increased understanding of the mechanisms by which LXR signalling regulates lipid homeostasis in different tissues (including the liver, intestine and brain), has highlighted new opportunities for therapeutic intervention in human metabolism. New strategies for the pharmacological manipulation of LXRs and their target genes offer promise for the treatment of human diseases in which lipids have a central role, including atherosclerosis and Alzheimer's disease.
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LXRs (LXRβ and LXRα) are nuclear hormone receptor transcription factors that drive transcriptional activation of Apoe, as well as other genes involved in cholesterol, fatty acid, and glucose metabolism.
“Liver-X receptors (LXRβ and LXRα) are members of the nuclear hormone receptor family of transcription factors that drive transcriptional activation of Apoe, as well as other genes involved in cholesterol, fatty acid, and glucose metabolism”
From LXR/ApoE Activation Restricts Innate Immune Suppression in Cancer (2018) · cites this paper as Hong and Tontonoz, 2014
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Self-citation
- Authors
- Hong, C., & Tontonoz, P.
- Affiliations
- Howard Hughes Medical Institute (US)
- Corresponding author
- Tontonoz, Peter
- Venue
- Nature Reviews Drug Discovery
- Published
- 2014-05-16
- Volume
- 13
- Issue
- 6
- Pages
- 433-444
- ISSN
- 1474-1776 (ISSN-L)
- 1474-1784
- OpenAlex
- W2081832076
- Cited by
- 587
- References
- 8
- Citations by year
- 2026: 26 · 2025: 35 · 2024: 39 · 2023: 37 · 2022: 42 · 2021: 54 · 2020: 50 · 2019: 68 · 2018: 73 · 2017: 52 · 2016: 60 · 2015: 47 · 2014: 4
- FWCI
- 10.32
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Nature Reviews Drug Discovery (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Howard Hughes Medical Institute
- National Heart, Lung, and Blood Institute (HL066088, R01HL066088)
- Topics
- Health Sciences › Medicine › Surgery › Cholesterol and Lipid Metabolism
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Peroxisome Proliferator-Activated Receptors
- Health Sciences › Medicine › Cardiology and Cardiovascular Medicine › Lipid metabolism and disorders
- Keywords
- liver X receptor, lipid homeostasis, cholesterol metabolism, tissue-specific gene regulation, therapeutic target, atherosclerosis, Alzheimer's disease, intestinal cholesterol transport, brain cholesterol metabolism, drug development
- MeSH terms
- Liver X Receptors, Alzheimer Disease, Animals, Hypolipidemic Agents, Brain, Clinical Trials as Topic, Drug Evaluation, Preclinical, Humans, Intestinal Mucosa, Intestines, Liver, Nerve Tissue Proteins, Neurons, Drug Design, Signal Transduction, Drugs, Investigational, Nootropic Agents, Protein Isoforms, Atherosclerosis, Lipid Metabolism, Drug Discovery, Orphan Nuclear Receptors, Molecular Targeted Therapy
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