Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor α
BB Busch, WC Stevens, R Martin… - Journal of medicinal …, 2004 - ACS Publications
BB Busch, WC Stevens, R Martin, P Ordentlich, S Zhou, DW Sapp, RA Horlick, R Mohan
Journal of medicinal chemistry, 2004•ACS PublicationsThe estrogen-related receptor α (ERRα) is an orphan receptor belonging to the nuclear
receptor superfamily. The physiological role of ERRα has yet to be established primarily
because of lack of a natural ligand. Herein, we describe the discovery of the first potent and
selective inverse agonist of ERRα. Through in vitro and in vivo studies, these ligands will
elucidate the endocrine signaling pathways mediated by ERRα including association with
human disease states.
receptor superfamily. The physiological role of ERRα has yet to be established primarily
because of lack of a natural ligand. Herein, we describe the discovery of the first potent and
selective inverse agonist of ERRα. Through in vitro and in vivo studies, these ligands will
elucidate the endocrine signaling pathways mediated by ERRα including association with
human disease states.
The estrogen-related receptor α (ERRα) is an orphan receptor belonging to the nuclear receptor superfamily. The physiological role of ERRα has yet to be established primarily because of lack of a natural ligand. Herein, we describe the discovery of the first potent and selective inverse agonist of ERRα. Through in vitro and in vivo studies, these ligands will elucidate the endocrine signaling pathways mediated by ERRα including association with human disease states.
ACS Publications