Ученые из Венгрии впервые показали, как препарат карипразин связывается с рецепторами мозга на атомном уровне

From Budapest to the World: How Cariprazine Changed Psychiatry—and Why Its Developers Deserve Olympic-Style Recognition.Continue reading An international research team led by scientists at the HUN-REN Center for Natural Sciences has for the first time shown at atomic resolution how cariprazine, a drug developed in Hungary, binds to the brain’s dopamine D3 receptor. The findings, published in the journal Science Advances, not only provide a better understanding of how a drug used around the world works but could also help in the development of new, more targeted psychiatric medications, HUN-REN said on its website. Cariprazine is one of the internationally significant achievements of Hungarian pharmaceutical research. It was discovered by researchers at Hungarian pharmaceutical company Gedeon Richter, and over the past decade it has been used to treat millions of patients worldwide living with schizophrenia and bipolar disorder. What makes the current research particularly significant is that decades after the drug molecule was discovered, scientists have now been able to precisely identify the molecular interactions that determine how it affects the dopamine D3 receptor. The study was led by György Miklós Keserű, a member of the Hungarian Academy of Sciences and a researcher at the HUN-REN Center for Natural Sciences, who was himself a member of the Richter research team involved in the discovery of cariprazine. This allowed him to follow the history of the same Hungarian-developed drug molecule from its original discovery to an understanding of its structure and function at the atomic level. Keserű said that following the success of cariprazine, the researchers have now been able to understand at the molecular level how the drug works at the dopamine D3 receptor. The significance of the findings goes beyond a more precise understanding of how cariprazine works. Based on the new structural information, the researchers also designed and validated compounds that target the dopamine D3 receptor more selectively than previous compounds. Greater selectivity could pave the way for medications that intervene more precisely in therapeutically important processes while causing fewer unwanted effects. The relationships uncovered in the study could therefore serve as a kind of structural blueprint for the rational design of new drug molecules. The newly designed compounds are currently research-stage results, and further preclinical and clinical studies will be needed to determine whether they could eventually become usable medications. The research could nevertheless open up new possibilities for developing drugs aimed at treating schizophrenia, bipolar disorder and other neuropsychiatric conditions. Brian Kobilka, an honorary member of the Hungarian Academy of Sciences and a Nobel Prize-winning pioneer in the field, described the findings as an exciting discovery that could hopefully contribute to the development of new drugs for treating complex psychiatric disorders. László Hunyady, vice president for life sciences of the Hungarian Academy of Sciences, also highlighted the significance of the work. He emphasized that the findings clearly demonstrate the important role that research conducted in Hungary’s academic sector can play in industrial pharmaceutical development. Researchers at the HUN-REN Center for Natural Sciences carried out the project together with international partners, including scientists from the Weizmann Institute of Science and the University of Nottingham. Via hun-ren.hu, Featured image: Pixabay