[HTML][HTML] Crystal structure of the human RORα ligand binding domain in complex with cholesterol sulfate at 2.2 Å

J Kallen, JM Schlaeppi, F Bitsch, I Delhon… - Journal of Biological …, 2004 - ASBMB
The retinoic acid-related orphan receptor α (RORα) is an orphan member of the subfamily 1
of nuclear hormone receptors. Our recent structural and functional studies have led to the
hypothesis that cholesterol or a cholesterol derivative is the natural ligand of RORα. We
have now solved the x-ray crystal structure of the ligand binding domain of RORα in complex
with cholesterol-3-O-sulfate following a ligand exchange experiment. In contrast to the 3-
hydroxyl of cholesterol, the 3-O-sulfate group makes additional direct hydrogen bonds with …