Description
SR1001 is an inverse agonist at RORα/γ receptors that prevents Th17 cell development, differentiation, and function. It exhibits anti-diabetic, anti-inflammatory, immunomodulatory, and antidepressant activities. In animal models of diabetes, SR1001 decreases diabetes incidence and insulitis, suppresses expression of pro-inflammatory cytokines, and increases levels of CD4+, Foxp3+ Treg cells. In animal models of depression-like behaviors, SR1001 decreases Th17-dependent learned helplessness.
References
Solt LA, Banerjee S, Campbell S, et al. ROR inverse agonist suppresses insulitis and prevents hyperglycemia in a mouse model of type 1 diabetes. Endocrinology. 2015 Mar;156(3):869-81. PMID: 25560829.
Beurel E, Harrington LE, Jope RS. Inflammatory T helper 17 cells promote depression-like behavior in mice. Biol Psychiatry. 2013 Apr 1;73(7):622-30. PMID: 23174342.
Solt LA, Kumar N, Nuhant P, et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature. 2011 Apr 28;472(7344):491-4. PMID: 21499262.
