On Target – New Research Improves Drug Targeting
Scientists have developed a novel technique to provide more precise information about whether a drug has hit its target, ultimately making the drug development cycle less costly and more efficient.
This new research offers the pharma industry a more precise tool to determine the effectiveness of many pharmaceuticals by ensuring that a drug reached its target protein in the human body. At present, drug developers can only theorise about whether a drug has reached its target protein, which can result in a long and costly process for developing drug and this new technique, called the Cellular Thermal Shift Assay (CETSA), has the potential to change this.
CETSA’s inventor, Professor Pär Nordlund from Nanyang Technological University’s School of Biological Sciences in Singapore explains that scientists face two challenges with drug targeting: how to identify the right proteins to target and how to design drug molecules which are able to efficiently seek out and bind to these proteins.
He points out that the new method will not only ease these two key problems, but also has important applications in monitoring a patient’s progress during treatment. “With CETSA, we can, in principle, determine which drug and treatment regime is most effective at targeting the proteins in the tumour in cancer patients, and monitor when resistance is developing,” says Prof Nordlund.
It is hoped that CETSA will assist drug scientists with taking away most of the existing usual trial-and-error guesswork from the drug development process. “By heating protein samples and finding out which proteins are ‘cooked’ and which are left ‘uncooked’ due it being more heat resistant, we are able to know if the drugs had reached their target cells and if it had caused the desired binding to the proteins, blocking its functions,” commented Nordlund.
"With CETSA, costly and challenging drug development cycles can potentially be made more efficient, as the method can be used as a stringent control step at many phases of the process. Other methods are available for indirect measurements of drug binding but they are often less accurate, and CETSA will be a valuable tool to complement these technologies," explains Nordlund.
The NTU team, along with collaborating researchers from Sweden’s Karolinska Institute and Linköping University, has recently published their findings in the highly respected international journal Science.
The work has taken this team three years to progress to this point and Nordlund says they are now in the process of developing a prototype device. They are also in talks with pharmaceutical companies who are interested to collaborate in further research.