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Chemical Screening of Nuclear Receptor Modulators
Mari Ishigami-Yuasa1, Hiroyuki Kagechika1
1Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University (TMDU), 2-3-10 Kanda-Surugadai, Chiyoda-ku, Tokyo 101-0062, Japan.
International Journal of Molecular Sciences
|August 6, 2020
Summary
Nuclear receptors regulate key biological processes. This review details chemical screening methods and libraries for discovering nuclear receptor modulators, essential for drug development.
Area of Science:
- Molecular Biology
- Pharmacology
- Biochemistry
Background:
- Nuclear receptors are crucial ligand-inducible transcription factors regulating homeostasis, metabolism, and proliferation.
- Their structural and functional similarities facilitate the study of their regulatory mechanisms.
- Modulators like agonists and antagonists are vital tools and drug candidates.
Purpose of the Study:
- To review chemical screening methods for identifying nuclear receptor modulators.
- To highlight assay systems and chemical libraries used in screening.
- To present recent examples of discovered nuclear receptor modulators.
Main Methods:
- Focus on diverse assay systems for evaluating nuclear receptor modulation.
- Discussion of chemical libraries utilized for high-throughput screening.
- Review of established and emerging screening methodologies.
Main Results:
- Availability of numerous assay systems for screening nuclear receptor modulators.
- Established chemical libraries provide diverse compound collections for screening.
- Recent discoveries showcase the efficacy of these screening approaches.
Conclusions:
- Chemical screening methods are indispensable for discovering nuclear receptor modulators.
- Assay systems and chemical libraries are key components in drug discovery pipelines.
- Continued development in screening technologies will accelerate the identification of novel modulators.
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