Journal
CHEMISTRY & BIOLOGY
Volume 19, Issue 1, Pages 51-59Publisher
CELL PRESS
DOI: 10.1016/j.chembiol.2011.12.011
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Funding
- NCI NIH HHS [R01 CA134873-03, R01 CA134873] Funding Source: Medline
- NIDDK NIH HHS [R01 DK080201, R24 DK089984, R24 DK089984-01, R01 DK080201-06] Funding Source: Medline
- NIMH NIH HHS [R01 MH092769, R01 MH092769-01] Funding Source: Medline
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The nuclear receptor (NR) superfamily is composed of 48 members in humans and includes receptors for steroid hormones, thyroid hormone, various lipids and oxysterols. This superfamily has been a rich source of drug targets for myriad diseases including inflammation, cancer, and metabolic disorders. Approximately half of the superfamily have well characterized natural ligands whereas the remaining receptors are considered orphan receptors and remain a focus of a number of investigators assessing their ability to be regulated by ligands. Here, we review recent discoveries that yield important insight into the druggability of three orphan nuclear receptors: the retinoic acid receptor-like orphan receptors (RORs), peroxisome proliferator-activated receptor gamma (PPAR gamma), and liver receptor homolog-1 (LRH-1).
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