A new antitumor substance was synthesized at the UrFU Center for Chemical and Pharmaceutical Technologies (Photo: Rodion Narudinov)
Chemists of the Ural Federal and Volgograd State Medical Universities have created a compound that suppresses the growth of cancer cells. A new powerful substance can become the basis for antitumor drugs, as it affects the pathology that leads to the development of such malignant tumors as breast, lung, prostate, and lymph node cancer. The description of the substance and the results of the experiments are published in the journal Molecules.
"It is known that type 2 casein kinase (SK2) suppresses apoptosis in cells, however, an increased content of type 2 casein kinase is observed in tumor cells, which indicates resistance to apoptosis of these cells compared to conventional ones. If you block this protein, you can achieve the death of tumor cells. So, our team managed to develop a universal approach to the synthesis of new azolopyrimidines and obtain a library of the corresponding heterocycles as potential type 2 casein kinase inhibitors," explains Grigory Urakov, an engineer at the UrFU Scientific Laboratory of Medicinal Chemistry and Advanced Organic Materials.
Casein kinase 2 is a type of protein kinase that plays an important role in the regulation of cell processes. It is believed that CK2 is involved in the appearance of diseases such as multiple sclerosis, inflammation, hypertension, viral infections. But the main thing is that CK2 has been proven to be a key regulator of cellular apoptosis (death) and a key element that suppresses oncogenesis (the transformation of normal cells into cancer cells). And by acting on the malfunction of CK2, it is possible to stop the development of the tumor.
"Today, a wide range of different molecules are known as CK2 inhibitors. These are polyhalogenated derivatives of benzimidazole and benzotriazole, nitrogen-containing heterocycles and their polycondensed analogues, as well as coumarin derivatives. However, most of the currently available CK2 inhibitors do not have the properties necessary for successful clinical trials. At the same time, our compound showed good activity with respect to inhibition of SC2 in the nanomolar range, which makes it possible to create analogues of these compounds," says Grigory Urakov.
Activity with respect to inhibition of SC2 in the nanomolar range means that less drug is required for treatment than existing analogues, that is, it is more effective, binds well to SC2. In addition, according to scientists, the new substance is a kind of "constructor" — it has modification centers. This means that, leaving the base, it is possible to change the design of the compound and obtain new substances, probably with greater activity or new properties.
Tests of substances for inhibition of casein kinase 2 took place in Volgograd. There, scientists tested them in vitro, on cells grown in the laboratory. The chemists' plans include further research of substances and improvement of the obtained compounds.
The information is taken from the portal "Scientific Russia" (https://scientificrussia.ru/), posted by Natalia Safronova
Information provided by the press service of the Ural Federal University
Photo source: urfu.ru
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