Endocrine Abstracts

Nuclear receptors are ligand-dependent transcription factors that govern complex physiologic pathways, including reproduction, development, and metabolism. The importance of this receptor superfamily is emphasized by its conservation throughout evolution, from simple multicellular organisms to humans. Because of their therapeutic potential in governing physiology and disease, targeting nuclear receptors for novel drug discovery has become a major interest in both academia and ...

The resin of the guggul tree (Commiphora mukul) has been used for millennia in Ayurvedic medicine to treat a variety of ailments. Extracts of this resin have been reported to lower LDL cholesterol in humans, and the plant sterol guggulsterone (4,17(20)-pregnadiene-3,16-dione) is thought to be the active agent. We have found that guggulsterone is an antagonist ligand for the nuclear the bile acid receptor, FXR. Guggulsterone treatment lowers hepatic cholesterol levels in wild t...