VATIS UPDATE Article

Researchers at the Indian Institute of Science (IISc), India, have synthesised a small molecule that shows a degree of promise as an anticancer agent. In particular, the inhibitor was effective against leukaemia. The work was done in collaboration with researchers from the University of Mysore. The molecule (a benzothiazole derivative), codenamed 5g, was found to be effective in inhibiting cell proliferation in both leukaemia and breast cancer cell lines.

This was achieved by arresting a particular phase (G2/M) of the cell cycle, thereby preventing cancer cells from dividing and growing in number. In the case of mouse models, the 5g molecule was able to arrest tumour growth without causing significant side-effects. The inhibitor was able to arrest the cancer cells from proliferating by elevating the levels of intracellular reactive oxygen species (ROS), which, in turn, causes DNA damage by breaking the DNA’s double-strands.

The molecule also activated the cell death pathway when higher concentration was used. However, the molecule did not cause any damage to normal blood cells. “Depending on the dosage, the molecule can either kill or cause DNA damage thus arresting normal cell cycle, or allow the cells to repair the DNA double-strand breaks and revert to normal cell cycle [at lower concentrations],” said Dr. Sathees C. Raghavan at IISc.