2014
DOI: 10.1038/aps.2014.120
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ROR nuclear receptors: structures, related diseases, and drug discovery

Abstract: 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) α, β and γ 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 synthe… Show more

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Cited by 118 publications
(84 citation statements)
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“…The subfamily of ROR orphan nuclear receptors have emerged as important regulators of metabolism and immune system. The structures, biology and related drug discovery targeting RORs have been intensively studied by academic and industrial groups, and are viewed by Zhang and coworkers [8] . Together, these articles provide an overall view on the converging roles of orphan nuclear receptors in metabolic regulation and their potential as drug targets for metabolic diseases.…”
Section: Editorialmentioning
confidence: 99%
“…The subfamily of ROR orphan nuclear receptors have emerged as important regulators of metabolism and immune system. The structures, biology and related drug discovery targeting RORs have been intensively studied by academic and industrial groups, and are viewed by Zhang and coworkers [8] . Together, these articles provide an overall view on the converging roles of orphan nuclear receptors in metabolic regulation and their potential as drug targets for metabolic diseases.…”
Section: Editorialmentioning
confidence: 99%
“…[120] Isoxazole derivatives have also been explored as retinoic acid receptor-related orphan receptor (ROR) ligands. [121] RORs are nuclear receptors (NRs) engaged in av ariety of biological processes like cell proliferation, differentiation, development and homeostasis. As such, they have been am ajor research themea sp rimary drug targets for many physiological as well as pathological processes.…”
Section: Psychoactive Drugs (Psychotropics)mentioning
confidence: 99%
“…Such small molecule therapeutics may provide broader and more potent therapeutic efficacy when compared to biologics targeting single cytokines in the RORγt pathway. 10 Identification of small molecule inhibitors of RORγt activity is of considerable interest. Several RORγ biased inverse agonist series were disclosed in literature in the last two years including the tertiary sulfonamides (1), 11 the phenanthridinones (2), 12 the aryl-amides (3a, 3b), 13 and the diphenylpropanamides (4), 14 scaffolds shown in Figure 1.…”
Section: Bioorganic and Medicinal Chemistry Lettersmentioning
confidence: 99%