- Discovery and optimization of a series of sulfonamide inverse agonists for the retinoic acid receptor-related orphan receptor-α
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Background: Despite a massive industry endeavor to develop RORγ-modulators for autoimmune disorders, there has been no indication of efforts to target the close family member RORα for similar indications. This may be due to the misconception that RORα is
- Doebelin, Christelle,He, Yuanjun,Campbell, Sean,Nuhant, Philippe,Kumar, Naresh,Koenig, Marcel,Garcia-Ordonez, Ruben,Chang, Mi Ra,Roush, William R.,Lin, Li,Kahn, Susan,Cameron, Michael D.,Griffin, Patrick R.,Solt, Laura A.,Kamenecka, Theodore M.
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p. 676 - 684
(2019/10/28)
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- MODULATORS OF THE RETINOIC ACID RECEPTOR-RELATED ORPHAN RECEPTORS
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The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as RORα RORβ, or RORγ. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.
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Page/Page column 6; 45; 46
(2011/10/10)
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