| 内容提要: |
The retinoic acid receptor-related receptors (RORs) are members of the nuclear receptor (NR) superfamily of transcription factors.RORs regulates inflammation, lipid metabolism, and cellular differentiation of several non-epithelial tissues.RORs are still characterized as orphan receptors since ligands have not yet been identified for these proteins.T0901317 (T1317) is the first synthetic ligand that binds to and modulates the activity of RORα and RORγ, but T1317 was originally identified as a LXR agonist and a receptor for bile acids FXR. SR1078 displayed a unique pharmacological profile indicating a high potential to be used as a chemical probe for assessment of ROR function. This work leading to the identification of SR1078
also demonstrates that it is possible to develop ROR selective synthetic ligands that lack activity at related receptors such as LXR and FXR. |