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Published on: March 14, 2020
The liver X receptors
1Pfizer Global Research and Development, Ann Arbor, MI 48105, USA. deepak.s.lala@pfizer.com
Abstract:
The liver X receptors (LXRs), members of the nuclear receptor superfamily, are potential targets for a variety of diseases. While there are many opportunities for the development of LXR-based therapeutics, there are some major hurdles, such as the ability of LXRs to cause hypertriglyceridemia, as well as some species-dependent aspects of LXR-mediated gene regulation. In addition to classical pharmacological approaches using relevant cellular and animal models, systematic molecular-based strategies will be important in overcoming these obstacles.
Insights
Liver X receptors (LXRs) are promising drug targets for various diseases. However, challenges like hypertriglyceridemia and species-specific gene regulation must be addressed for effective LXR-based therapeutics.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Liver X receptors (LXRs) are nuclear receptors implicated in various physiological processes.
- LXRs represent potential therapeutic targets for a range of diseases.
Purpose of the Study:
- To discuss the therapeutic potential of LXRs.
- To highlight the challenges and strategies for developing LXR-based drugs.
Main Methods:
- Review of existing literature on LXR function and pharmacology.
- Analysis of LXR-mediated gene regulation and associated adverse effects.
Main Results:
- LXR activation offers therapeutic opportunities but is associated with hypertriglyceridemia.
- Species-dependent differences in LXR gene regulation present a hurdle for drug development.
Conclusions:
- Overcoming challenges in LXR drug development requires both classical and molecular strategies.
- Further research into LXR mechanisms is crucial for advancing LXR-based therapeutics.
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