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Targeting liver X receptors in cancer therapeutics
Chin-Yo Lin1, Jan-Åke Gustafsson2
1Center for Nuclear Receptors and Cell Signaling, Department of Biology and Biochemistry, University of Houston, Houston, Texas 77204-5056, USA.
Abstract:
Members of the nuclear receptor superfamily of ligand-dependent transcription factors carry out vital cellular functions and are highly druggable therapeutic targets. Liver X receptors (LXRs) are nuclear receptor family members that function in cholesterol transport, glucose metabolism and the modulation of inflammatory responses. There is now accumulating evidence to support the involvement of LXRs in a variety of malignancies and the potential efficacy of their ligands in these diseases. This Review summarizes the discovery and characterization of LXRs and their ligands, their effects and mechanisms in preclinical cancer models, and the future directions of basic and translational LXR research in cancer therapeutics.
Insights
Liver X receptors (LXRs) are key regulators of cellular processes. Emerging research highlights their role in cancer, showing potential for LXR ligands as novel cancer therapeutics.
Area of Science:
- Molecular biology
- Endocrinology
- Oncology
Background:
- Nuclear receptors are critical transcription factors with significant therapeutic potential.
- Liver X receptors (LXRs) regulate cholesterol, glucose, and inflammation.
- Growing evidence links LXRs to various cancers.
Purpose of the Study:
- To review the discovery and characterization of LXRs and their ligands.
- To summarize LXR effects and mechanisms in preclinical cancer models.
- To outline future directions for LXR research in cancer therapeutics.
Main Methods:
- Literature review of LXR discovery and characterization.
- Analysis of preclinical cancer models investigating LXR activity.
- Synthesis of current understanding of LXR mechanisms in cancer.
Main Results:
- LXRs are involved in diverse cellular functions beyond their established roles.
- LXR ligands demonstrate therapeutic potential in preclinical cancer studies.
- Specific mechanisms of LXR action in different cancer types are being elucidated.
Conclusions:
- LXRs represent a promising target for cancer therapy.
- Further research is needed to translate preclinical findings into clinical applications.
- Targeting LXRs offers a novel strategy for modulating cancer progression and treatment.
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