Journal
ACTA PHARMACOLOGICA SINICA
Volume 36, Issue 1, Pages 71-87Publisher
ACTA PHARMACOLOGICA SINICA
DOI: 10.1038/aps.2014.120
Keywords
nuclear receptor; retinoic acid receptor-related orphan receptor; autoimmune disease; metabolic disorder; rational drug design
Funding
- National Natural Science Foundation of China [81373325]
- National Key Basic Research Program of China (973 Program) [2013CB910601]
- CAS
- Guangzhou Bureau of Science and Information Technology, China [2012Y2-00051, 2013Y200048]
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Nuclear receptors (NRs) are ligand-regulated transcription factors that regulate metabolism, development and immunity. The NR superfamily is one of the major classes of drug targets for human diseases. Retinoic acid receptor-related orphan receptor (ROR) alpha, beta and gamma belong to the NR superfamily, and these receptors are still considered as 'orphan' receptors because the identification of their endogenous ligands has been controversial. Recent studies have demonstrated that these receptors are regulated by synthetic ligands, thus emerge as important drug targets for the treatment of multiple sclerosis, rheumatoid arthritis, psoriasis, etc. Studying the structural basis and ligand development of RORs will pave the way for a better understanding of the roles of these receptors in human diseases. Here, we review the structural basis, disease relevance, strategies for ligand identification, and current status of development of therapeutic ligands for RORs.
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