Liver X receptors: From pharmacology to nanoparticle-based drug delivery
Open accessAbstract
Liver X receptors (LXRs) are master regulators of various biological processes, including metabolism, inflammation, development, and reproduction. As well-known nuclear oxysterol receptors of the nuclear receptor (NR) family, LXRs have two homologous subtypes, LXRα (NR1H3) and LXRβ (NR1H2). Since the mid-1990s, numerous LXR-targeted drugs have been designed to treat diseases such as atherosclerosis, systemic lupus erythematosus, and cancer. These modulators include agonists and antagonists, and the selectivity of them have been development from diverse aspects, including subtype-specific, cell-specific, tissue-specific types. Meanwhile, advanced delivery systems are also exploreed to facilitate the application of LXR drugs in clinical setting. One of the most promising delivery systems involves the use of nanoparticles and is expected to increase the clinical potential of LXR modulators. This review discusses our current understanding of LXR biology and pharmacology, focusing on the development of modulators for LXRα and/or LXRβ, and the nanoparticle-based delivery systems for promising LXR modulators with potential for use as drugs.
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LXR agonists reduce lipid droplet accumulation through enhanced cholesterol efflux and exhibit anti-inflammatory properties, but their concurrent promotion of lipogenesis also leads to adverse effects such as hepatic steatosis and hyperlipidemia.
“For example, liver X receptor (LXR) agonists reduce LD accumulation through enhanced cholesterol efflux and exhibit anti-inflammatory properties, but their concurrent promotion of lipogenesis also leads to adverse effects such as hepatic steatosis and hyperlipidemia.82,83”
From Amyloid-β induces lipid droplet-mediated microglial dysfunction via the enzyme DGAT2 in Alzheimer’s disease (2025) · cites this paper as [83]
Cites
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Prakash, P., Manchanda, P., Paouri, E., Bisht, K., Sharma, K., Rajpoot, J., Wendt, V., Hossain, A., Wijewardhane, P. R., Randolph, C. E., et al. (2025) · Immunity · doi:10.1016/j.immuni.2025.04.029 · Cited by 104 · see citing works
- Authors
- Hua, X., & Wei, X.
- Affiliations
- King's College London (GB)
- Wenzhou Medical University (CN)
- Corresponding author
- Wei, Xiduan
- ORCID
- Wei, Xiduan
- Venue
- European Journal of Pharmacology
- Publisher
- Elsevier BV
- Published
- 2023-10
- Volume
- 956
- Pages
- 175953
- ISSN
- 0014-2999 (ISSN-L)
- OpenAlex
- W4385491068
- Cited by
- 14
- References
- 4
- Citations by year
- 2026: 5 · 2025: 6 · 2024: 3
- FWCI
- 0.91
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- European Journal of Pharmacology (publishedVersion, cc-by)
- PubMed (publishedVersion)
- 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 › Oncology › Drug Transport and Resistance Mechanisms
- Keywords
- liver X receptor, liver X receptor alpha, LXRβ, nanoparticle drug delivery, atherosclerosis, systemic lupus erythematosus, cancer, drug delivery systems
- MeSH terms
- Liver X Receptors, Humans, Atherosclerosis, Orphan Nuclear Receptors
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