Key Points
- Osaka University developed a new drug screening method using single-molecule tracking to accelerate discovery.
- The technique tracks how target molecules in cells respond to various drugs, validating its use with the EGFR target.
- The research team identified seven previously unknown drugs affecting EGFR, suggesting new treatment options.
- Researchers aim to apply this method to discover drugs targeting other disease-related receptors, potentially speeding up drug development.
A research team from Osaka University has unveiled a groundbreaking drug screening technology that rapidly identifies potential drugs by tracking molecule behavior within cells. This innovative method, which centers on single-molecule imaging, was validated using the epidermal growth factor receptor (EGFR) — a key target in cancer therapy — successfully identifying established and previously unrecognized drugs that affect EGFR. This advancement holds promise for accelerating drug discovery and repurposing existing medications for new therapeutic applications.
Drug discovery typically involves identifying cellular molecules driving disease progression and screening for drugs that can inhibit these targets. However, the screening process can be complex and time-intensive. Osaka University researchers developed a single-molecule tracking technique to streamline this process to observe how candidate drugs affect a specific target molecule in cells. Their approach, detailed in a study published in Nature Communications, employs an advanced imaging system known as AiSIS (Artificial Intelligence Single-Molecule Imaging System), which enhances screening speeds by approximately 100-fold compared to traditional manual methods.
To verify their new technique, the team conducted screenings targeting EGFR, a molecule integral to the growth and spread of various cancers, including lung cancer. Since multiple existing drugs block EGFR as part of cancer treatment, it provided an ideal benchmark to assess the effectiveness of the Osaka University screening method. Using a library of over 1,000 approved drugs, the researchers successfully identified all existing EGFR-targeting drugs. More significantly, they discovered seven additional drugs previously unrecognized as EGFR influencers, opening avenues for potential cancer therapies.
The single-molecule imaging system enables scientists to monitor EGFR’s behavior in real-time, observing how it responds to each drug. This includes tracking processes like assembling and disassembling target molecules, known as multimer formation, which plays a critical role in cellular signaling pathways.
“Our single-molecule imaging technique allows us to directly observe how biomolecules move and interact in cells, introducing a new approach to drug discovery,” explained Masahiro Ueda, senior author of the study. “This could help us develop drugs with unique mechanisms of action and identify new uses for existing drugs.”
With successful validation using EGFR, the Osaka team now plans to apply their technology to screen drugs targeting other receptors involved in diseases. This technique could transform drug discovery by quickly identifying candidate drugs for conditions that are challenging to treat, potentially improving patient outcomes with faster, more targeted therapies.
