Recent studies show that enhanced mitochondrial biogenesis can “fuel” the cancer cells to
grow and migrate. It is therefore proposed that inhibiting the mitochondrial biogenesis could be a new
approach to cancer therapy. This review summarizes recent patents and papers in the development of
small molecule inhibitors of key regulators responsible for tumor mitochondrial biogenesis, including
PPARγcoactivator-1α(PGC-1α), PPARγcoactivator-1β, estrogen-related receptor family (ERRs),
estrogen receptor α(ERα), mammalian target of rapamycin, c-Myc and PPARs.