Technological breakthrough paves the way for better drugs

Researchers at Karolinska Institutet in Sweden have developed the first method for directly measuring the extent to which drugs reach their targets in the cell. The method, which is described in the scientific journal Science, could make a significant contribution to the development of new, improved drug substances, reports EurekAlert.

Most drugs operate by binding to one or more proteins and affecting their function, which creates two common bottlenecks in the development of drugs; identifying the right target proteins and designing drug molecules able to efficiently seek out and bind to them. No method has been available for directly measuring the efficiency of the drug molecules to locate and bind to its target protein. Now researchers from Karolinska Institutet have developed a new tool called CETSA (Cellular Thermal Shift Assay), which utilize the concept that target proteins usually get stabilized when drug molecules bind.

"We have shown that the method works on a wide variety of target proteins and allows us to directly measure whether the drug molecules reach their targets in cells and animal models," says lead investigator Par Nordlund, a professor at the Department of Medical Biochemistry and Biophysics, adding: "We believe that CETSA will eventually help to improve the efficiency of many drugs and contribute to better drug molecules and more successful treatments."