ERRα - A central regulator of energy metabolism


The estrogen-related receptor α (ERRα), a nuclear receptor, is a central regulator of energy metabolism. In breast, prostate, and colon cancer, ERRα levels correlate with poor prognosis. ERRα also seems to be involved in the etiology of metabolic disorders, such as type 2 diabetes and metabolic syndrome. As an example, ERRα-deficient mice are resistant to high-fat diet-induced obesity and an inverse agonist of ERRα improves the metabolic profile in animal models of diabetes and obesity. However, existing compounds are either covalent binders resulting in safety problems or non-covalent binders with weak potency, false positives and a steroidal mode of action.


Lead Pharma is developing potent, non-covalent, non-steroidal inverse agonists with first-in-class potential for the treatment of various conditions, e.g. triple negative breast cancer or metabolic disorders.