A Fer/FerT inhibitor shows anti-cancer activity in vitro and in vivo

A team of researchers headed by Professor Uri Nir at Bar-Ilan University has developed a compound that inhibits enzymes critical for the survival of cancer cells. The compound has anti-cancer activity both in vitro and in vivo.

The intracellular tyrosine-kinase, Fer, is ubiquitously expressed in the body and is a key regulator of cell adhesion function. A large body of evidence suggests that Fer is implicated in malignant progression. Besides, a truncated variant of Fer, named FerT, has also been found to accumulate in cancer cells, and FerT inhibition impairs cancer cell proliferation and survival.

In 2014, Professor Nir and his team discovered that Fer and FerT populate the mitochondria of colon carcinoma cells, and guided mitochondrial accumulation of FerT in non-cancerous cells causes these cells to get tumor-forming capacity in vivo. Based on the findings, the researchers proposed that Fer and FerT could support tumor development through their mitochondrial functions.

Mitochondria are the powerhouse of the cell. They produce energy that every cell needs to survive. In cancer, mitochondria undergo reprogramming. Fer and FerT appear to be key players in mitochondrial reprogramming in cancer cells. Thus, targeting Fer or FerT is a potential therapeutic approach.

In the latest study, Professor Nir's team sought to find a selective inhibitor of Fer and FerT. Using an optimized yeast-based system, they screened tens of thousands of synthetic compounds. With the help of many other experimental techniques, the team finally identified a candidate inhibitor, termed E260.

To characterize the efficacy of E260, they tested it in human colon carcinoma cell lines and mice transplanted with human colon carcinoma cells. The results were encouraging. E260 evoked necrotic death in colon carcinoma cells in vitro. Importantly, E260 had no remarkable effect on the glycolytic rate in normal human cells. Treatment with E260 significantly attenuated tumor progression in tumor-bearing mice.

In summary, the new study identifies a Fer/FerT inhibitor with the potential to kill malignant cells without affecting normal cells. The researchers have concluded their findings in a paper published online in Nature Communications.
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