Estrogen receptor-related receptors α and γ as targets for drug discovery

MEDI 276

William J. Zuercher, william.j.zuercher@gsk.com, James M. Way, Andrew N. Billin, Aaron B. Miller, Lisa A. Orband-Miller, Robert T. Nolte, Liping Wang, and Timothy M. Willson. Discovery Research, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709
The estrogen receptor-related receptors (ERRs) are a subfamily of three nuclear receptors (NRs) which are most closely related to the classical estrogen receptors (ERs). Although they were among the first orphan NRs to be identified, many of the physiological roles and potential therapeutic applications of the ERRs await further elucidation. Herein we describe the identification and application of ERRα and ERRγ chemical tools in the investigation of the receptors as targets for drug discovery.