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Genomics versus orphan nuclear receptors--a half-time report
Timothy M Willson1, John T Moore
1GlaxoSmithKline, Discovery Research, Research Triangle Park, North Carolina 27709, USA. tmw20653@gsk.com
Molecular Endocrinology (Baltimore, Md.)
|June 1, 2002
Summary
Genomic technologies have advanced the study of human nuclear receptors, including orphan receptors. This progress identifies new pharmaceutical targets for treating human diseases.
Area of Science:
- Molecular Biology
- Genomics
- Endocrinology
Background:
- The 21st century began with a complete understanding of human nuclear receptors.
- Many nuclear receptors are ligand-activated transcription factors for hormones like steroids, retinoids, and thyroid hormones.
- Orphan nuclear receptors have poorly understood ligands and functions.
Purpose of the Study:
- To review the impact of genomics on deciphering orphan nuclear receptor functions.
- To highlight the identification of orphan nuclear receptors as pharmaceutical drug targets.
Main Methods:
- Application of chemical genomics.
- Application of structural genomics.
- Application of functional genomics.
Main Results:
- Genomic technologies have significantly aided in deciphering orphan nuclear receptor functions.
- Over half of the nuclear receptor gene family has undergone functional analysis.
- Several orphan nuclear receptors are emerging as pharmaceutical targets for human diseases.
Conclusions:
- Genomics has been instrumental in advancing the functional analysis of nuclear receptors.
- Orphan nuclear receptors represent promising targets for novel therapeutic strategies.