293753-88-5Relevant academic research and scientific papers
Modulators of retinoid-related orphan receptor gamma
-
Page/Page column 29; 38; 39, (2013/03/26)
Methods for modulating (inhibiting or stimulating) retinoid-related orphan receptor γ (RORγ) activity. This modulation has numerous effects, including inhibition of TH-17 cell function and/or TH-17 cell activity, and inhibition of re-stimulation of TH-17 cells, which are beneficial to treatment of inflammation and autoimmune disorders. Stimulation of RORγ results in stimulation of TH-17 cell function and/or activity which is beneficial for immune-enhancing compositions (e.g., vaccines).
Structure-based design of substituted hexafluoroisopropanol- arylsulfonamides as modulators of RORc
Fauber, Benjamin P.,De Leon Boenig, Gladys,Burton, Brenda,Eidenschenk, Celine,Everett, Christine,Gobbi, Alberto,Hymowitz, Sarah G.,Johnson, Adam R.,Liimatta, Marya,Lockey, Peter,Norman, Maxine,Ouyang, Wenjun,Rene, Olivier,Wong, Harvey
, p. 6604 - 6609 (2014/01/06)
The structure-activity relationships of T0901317 analogs were explored as RORc inverse agonists using the principles of property- and structure-based drug design. An X-ray co-crystal structure of T0901317 and RORc was obtained and provided molecular insight into why T0901317 functioned as an inverse agonist of RORc; whereas, the same ligand functioned as an agonist of FXR, LXR, and PXR. The structural data was also used to design inhibitors with improved RORc biochemical and cellular activities. The improved inhibitors possessed enhanced selectivity profiles (rationalized using the X-ray crystallographic data) against other nuclear receptors.
