Estrogen-related receptor α as a therapeutic target

The utility of nuclear receptors (NRs) as targets for drug discovery is well recognized. Growing evidence suggests that ERR(x, an orphan NR whose physiological and pathological roles remain under investigation, may have utility in the treatment of various cancer types as well as metabolic and osteopenic disorders. In this article, we review the literature on ERR alpha as a potential therapeutic target. Within this context we identify several key challenges in progressing small molecules which target ERR alpha, including the separation of efficacy and liability.