The researchers are confident that they will find new drugs that are effective against the most serious cancers and have few side effects, since the method does not interfere with the basic mechanisms of cell division, like today's chemotherapy interventions, but instead restores the physiologically normal state.

A revolutionary new approach to the treatment of cancers linked to RAS protein mutations has been born: ELTE researchers have found well-binding small molecules that do not interfere with the basic mechanisms of cell division, but rather restore a healthy state.

A significant number of cancers in humans are related to changes in genetic material, DNA mutations. More than 600 cancer-causing mutations are currently known, the most important of which are mutations of the RAS protein, which are found in 30 percent of all human tumors.

The most difficult-to-treat human carcinomas (adenocarcinomas of the lung, colon and pancreas) can be linked to them, ELTE wrote in a statement sent to MTI on Monday.

For about 30 years, researchers have been trying to attach inhibitory small molecules to mutant RAS proteins, but until recently with little success.

Recently, it was possible to find molecules (ARS-853, ARS-1620) that bind covalently, i.e. very strongly, to the RAS protein, but most drug molecules (such as the antibiotics used today) do not bind covalently to the target molecule, so ARS molecules are not optimal drug candidates - they explained.

According to the announcement

in the latest research of the ELTE PIT Bioinformatics Group led by Professor Vince Grolmusz, he proposed a revolutionary new approach to the treatment of cancers linked to RAS protein mutations.

Mutations in RAS prevent the GAP protein from binding to the RAS molecule, thereby allowing unrestricted cell division, thus the disease. According to ELTE researchers, molecules are therefore needed that glue the RAS and GAP molecules together. These can be found by looking for good "glue" small molecules between RAS and GAP molecules located in close proximity.

ELTE researchers, in extensive cooperation with several domestic institutions (KINETO Lab Kft., National Oncology Institute, Semmelweis University, Budapest University of Technology, HUN-REN Institute of Molecular Life Sciences, Uratim Kft.) have proven that potent drug candidate molecules can be found using the new approach.

The description of the new molecules and proof of their effectiveness was published on February 22 in the International Journal of Molecular Sciences. The preliminary results show that the best two small "glue" molecules found based on the new Hungarian method compete with the best similar molecules found so far in the world.

"The researchers are confident that by continuing the work, they will find new drugs that are effective against the deadliest cancers and have few side effects, since the method does not interfere with the basic mechanisms of cell division, like today's chemotherapy interventions, but restores the physiologically normal state"

- they wrote in the statement.

MTI

Source: https://www.elte.hu/content/forradalmian-uj-megkozelites-szuletett-a-legsulyosabb-rakok-gyogyitasara.t.30032

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