04 March 2020

Telomerase inhibitor

A cure has been found against the immortality of cancer cells

Svetlana Maslova, Hi-tech+

Treatment is aimed at the enzyme telomerase, the activity of which allows malignant cells to divide indefinitely. This target has been the target of scientists for decades. A new study by American scientists shows that there is a way to suppress the critical mechanism of immortality of cancer cells.

Telomerase is the main enzyme that allows cancer cells to live forever. It is found in more than 90% of human cancer cells and remains one of the main objects in the study of the nature of cancer. Scientists from Northwestern University have developed a molecule that can suppress the activity of the enzyme.

Article by Betori et al. Targeted Covalent Inhibition of Telomerase is published in the journal ACS Chemical Biology – VM.

The NU-1 compound is a small molecule that binds to telomerase and disables its activity. Without treatment, when a tumor develops, telomerase copies telomeres – the "tips" of DNA – many times, lengthening them. Thus, cells become immortal, since the natural process of telomere shortening is disrupted, which should gradually lead to cell death.

Scientists have been searching for NU-1 for more than ten years, testing various compounds, the source of which was the substance chromactomycin.

This substance is produced by bacteria and its ability to suppress telomerase was previously discovered.

Of more than 200 compounds, NU-1 proved to be the most effective. Its synthesis in the laboratory takes less than five steps, the authors specified.

Inhibition-of-Telomerase.jpg

In the center is the structural formula NU–1, attached to the telomerase molecule, in the gray ring are the mechanisms of action of telomerase, providing cancer cells with immortality. Figure from the press release of Northwestern University Chemists inhibit a critical gear of cell immortality – VM.

Another advantage of NU-1 is the molecular structure of the substance, which allows scientists to add additional therapeutic molecules to it.

"Our mechanism offers a new pathway in the treatment of cancer, and also opens up a new understanding of cellular aging," concluded the author of the study, scientist Karl Scheidt.

The current results were obtained as part of experiments on human cell cultures. Now scientists intend to strengthen the effect of NU-1 and test the treatment on animals.

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