Researchers Find A Way Of Developing More Efficient Drugs

Researchers have developed a way of directly measuring how efficient drugs are in reaching their targets, which could lead to the development of new and improved drug substances.

The study, by researchers at Karolinska Institutet in Sweden, has led to the development of a tool called CETSA (Cellular Thermal Shift Assay).

According to researchers, most drugs operate by binding to one or more proteins to affect their function. This has created problems when attempting to identify the correct target proteins and designing drug molecules that are able to search for and bind to its target proteins.

CETSA works by using the idea that target proteins are usually stabilized once drug molecules bind. Professor Pär Nordlund of the Department of Medical Biochemistry and Biophysics and lead investigator of the study, explained:

“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.

“We believe that CETSA will eventually help to improve the efficiency of many drugs and contribute to better drug molecules and more successful treatments.”

Previous studies have looked at ways of potentially improving drug efficiency. A study from Uppsala University, published in the journal Angewandte Chemie, revealed the concept of a polypeptide consisting of 42 amino acids to which virtually any target-seeking organic molecule can be bound.

Within this most recent study, the researchers also analyzed the processes in which cells in the body can become resistant to drugs.

During some clinical trials on humans, it has been revealed that some some drug molecules are unable to find the correct protein. The researchers believe that CETSA has the ability to predict whether existing drugs are suitable for certain patients.

Project team leader Daniel Martinez Molina of the Department of Medical Biochemistry and Biophysics aims to initiate the use of CETSA for patient studies. He said:

“We believe that the method can provide an important diagnostic tool in the treatment of cancer, for example, as CETSA can, in principle, enable us to determine which drug is most effective at targeting the proteins in the tumor.

“This also makes it possible for clinicians to ascertain at an early stage of treatment whether the tumor has developed a certain kind of resistance and which type of therapy could then be more suitable for the patient.”