Researchers have made a significant breakthrough by developing a technology that enables precise editing of individual atoms to enhance drug effectiveness.
This innovative technique, known as single-atom editing, is seen as a transformative advancement in drug development, allowing for quick and straightforward modifications of essential atoms that influence drug efficiency. The KAIST research team has achieved a world-first in this area.
On October 8th, KAIST, represented by President Kwang-Hyung Lee, announced that Professor Yoonsu Park and his research team from the Department of Chemistry have successfully created technology that allows for the efficient editing of oxygen atoms in furan compounds, turning them into nitrogen atoms. This transformation converts these compounds into pyrrole structures, which are extensively used in medications.
This groundbreaking research was published in the scientific journal Science on October 3rd, under the title “Photocatalytic Furan-to-Pyrrole Conversion.”
Many pharmaceutical drugs possess intricate chemical structures, yet their effectiveness can hinge on just one crucial atom. Elements such as oxygen and nitrogen are vital in enhancing the pharmacological properties of drugs, especially in combatting viral infections.
This important concept, called the “Single Atom Effect,” refers to how introducing specific atoms into a drug molecule can significantly alter its effectiveness. Therefore, identifying atoms that enhance drug performance is essential for advanced drug development.
Traditionally, analyzing the Single Atom Effect relied on lengthy and expensive synthesis operations because selectively editing single atoms in stable ring structures containing oxygen or nitrogen has proven challenging.
Professor Park’s team addressed this issue by introducing a photocatalyst that harnesses light energy. They designed a photocatalyst that functions like “molecular scissors,” which can easily cut and bond five-membered ring structures, allowing for single-atom edits at room temperature and atmospheric pressure—making it a global first.
The research team uncovered a new reaction mechanism where the activated molecular scissors remove oxygen from furan through single-electron oxidation and then sequentially introduce a nitrogen atom.
Donghyeon Kim and Jaehyun You, primary authors of the study and participants in KAIST’s combined master’s and doctoral program in Chemistry, noted that this method is highly adaptable since it utilizes light energy instead of extreme conditions. They also pointed out that this technology supports selective editing, even for complex natural products or pharmaceuticals. Professor Yoonsu Park, who spearheaded the research, expressed, “This significant advancement, which facilitates the targeted editing of five-membered organic ring structures, will pave the way for creating libraries of drug candidates, addressing a major hurdle in pharmaceutical development. I am hopeful this foundational technology will revolutionize how drugs are developed.”
The importance of this research was emphasized in the Perspective section of Science, where an esteemed external peer offers insights on impactful scientific studies.
This research received support from the Creative Research Program of the National Research Foundation of Korea, the Cross-Generation Collaborative Lab Project at KAIST, and the POSCO Science Fellowship from the POSCO TJ Park Foundation.
