ERRα
The estrogen-related receptor α (ERRα) is a nuclear receptor and a transcriptional master regulator of mitochondrial function and flexibility. ERRα upregulation and activation is associated with poor prognosis, recurrence of cancer, therapy resistance as well as with metastasis of several tumor types including melanoma, esophagus, breast and colon cancer.
ERRα inverse agonists, very much a first-in-class project, have a dual mechanism of action: 1) Inhibition of ERRα and ERRα-regulated adaptive OXPHOS, preventing disease progression, therapy resistance to targeted therapies and radiation and metastasis; 2) Reinvigoration of immunity.
Lead Pharma has developed the very first drug-like series of potent, non-covalent, non-steroidal ERRα inverse agonists.
