New technology optimizes drug discovery through single-molecule tracking

The discovery of new medicines is a crucial step in improving patients' lives. First, researchers need to identify molecules in the body's cells that cause disease, as these represent potential targets for new drugs. The next step is to evaluate possible drugs that can achieve these goals. However, screening can be a challenging and time-consuming process.

In a new study published in Nature communicationA team at Osaka University has developed a technology that streamlines drug discovery using single-molecule tracking. This method allows researchers to study the effects of many different drug candidates on a single target molecule. Built on the team's large-scale single-molecule intracellular imaging system, called AiSIS, the technology tests new drugs 100 times faster than traditional manual techniques.

The team tested their new method for screening drugs that can target the epidermal growth factor receptor (EGFR), a molecule that is central to the development and progression of various types of cancer. Since several drugs that block EGFR are already available to treat lung cancer, this was a good way to see how well their screening approach worked.

To validate our screening method, we used a library of over 1,000 approved drugs. We successfully identified all drugs known to target EGFR that are currently used to treat cancer patients. More importantly, we found that the library contained seven drugs that were not previously known to affect EGFR.”

Daisuke Watanabe, lead author of the study

The new imaging technique visualizes the behavior of EGFR after treatment with each drug, allowing researchers to study how it responds. For example, it is now possible to observe changes in the assembly and breakdown of target molecules in response to drug treatment, a process known as multimer formation.

“Screening using single-molecule imaging offers a new way to discover drugs by observing the movement of biomolecules in cells and the formation of multimers,” explains senior author Masahiro Ueda. “This has not been used for drug discovery before, and it means we should be able to develop new drugs with different mechanisms of action and even use already approved drugs for new targets.”

Because this study showed that the researchers' method using the known EGFR target worked as expected, they can now use this approach to test drugs that could potentially hit a number of other receptor targets that are closely involved in development and progression involved in the disease.