Science: the effect of drug binding target protein can be directly measured for the first time

Scientists at Karolinska Medical College in Sweden have developed a method that can directly measure the effect of drugs reaching their target proteins in cells for the first time, science and Technology Daily reported on July 5 (Beijing time) The new technology described in science will be a major contribution to the development of new and improved APIs Most drugs work by binding with one or more proteins and affecting their functions, but drug development also faces two common problems: identifying the right target proteins, and designing drug molecules that can effectively identify and bind them There is no way to directly measure the efficiency of drug molecular localization and binding its target protein before, which makes many stages of drug development process have a certain degree of uncertainty In some cases, the candidate drugs fail to achieve the expected effect in human clinical trials, which is proved to be caused by the drug molecules not combining with the correct proteins Researchers at Karolinska School of medicine have developed a new technology called cetsa (cell heat transfer analysis) based on the idea that the target protein usually becomes stable when it binds to drug molecules They believe that this technology can be used as an important control stage in the drug development process, as well as a supplement to other methods "We have shown that this method can be applied to a variety of target proteins, enabling us to directly measure whether the drug molecule has reached its target in the cell or animal model." "We believe that cetsa technology will eventually help to improve the efficiency of many drugs and help to develop better drug molecules and more effective treatment options," said pal nordelonde, chief researcher of the Department of medical biochemistry and Biophysics at the school of medicine The researchers also scrutinized processes that could lead to cell resistance and said the technology could determine whether existing drugs are suitable for individual patients, so it has potential value for personalized treatment "We believe that this method can provide an important diagnostic tool for cancer treatment For example, in principle, cetsa technology allows us to determine which drugs are most effective for proteins in tumors, and clinicians can also determine at the early stage of treatment whether tumors have some resistance and which treatment scheme is more suitable for patients." Nordlund's colleague Daniel Martinez Molina said his team is working on a project to use cetsa technology in patient research Editor in chief circle Body temperature can be measured, bone density can be measured, and even the effect of drug binding target protein can be measured directly, which makes people have to lament the rapid development of medical technology The cell heat transfer analysis technology mentioned in this paper, just like the sniper's sight, can help the sniper to adjust his position so as to hit the target more accurately In this way, it can not only improve the efficacy, but also reduce the side effects as much as possible The diagnosis and treatment method of "killing a thousand enemies and damaging eight hundred by oneself" may become the past, and those originally considered incurable diseases may meet with each other.