Development of novel Gemini-cholesterol analogues for retinoid-related orphan receptors

Abstract

Retinoic-acid-related Orphan Receptors (RORs) regulate the maintenance of the circadian rhythm and immune response among others and are involved in increasing numbers of pathologies including autoimmune diseases, cancer and neurological disorders leading to huge interest in the development of ROR ligands. Here, we describe the synthesis of six novel Gemini cholesterol analogues and the binding mode of one of them to RORγ.