Recently, scientists from Saint Louis firstly identified that a unique target which is very different from other counterparts. It is a drug which is targeting Warburg and may block the energy source of cancer to prevent cancer cells’ growth. This study was published in Cancer Cell.

Metabolism in cancer cells is primarily glycolytic even when oxygen is abundant. Aerobic glycolysis or the Warburg effect is well characterized and has been shown to be driven by mitochondrial defects, oncogenic stimuli, hypoxia, and aberrantly enhanced expression of glycolytic enzymes. In particular, elevated glycolytic gene expression is pervasive in cancers of the breast, colon, prostate, and lung.

A number of small molecules that target the Warburg effect and lipgenesis have been developed but none have become clinical treatments of off-target effects such as excessive weight loss, anorexia, high toxicity, and low efficacy in vivo.

In this study, researchers describe the anti-cancer properties of an LXR inverse agonist SR9243. Unlike previously developed targeted treatments, SR9243 selectively induces apoptosis in cancer cells but spares non-malignant tissues, exhibiting significant anti-tumor activity without overt toxicity, inflammation, or weight loss. The favorable safety profile of SR9243 demonstrates that LXR inverse agonists hold significant promise as prospective clinical treatments.