In pioneering drug development, the new technology that enables the easy and rapid editing of key atoms responsible for drug efficacy has been regarded as a fundamental and groundbreaking technology, revolutionizing the process of discovering potential drug candidates. KAIST researchers have become the first in the world to successfully develop single-atom editing technology that maximizes drug efficacy. Professor Yoonsu Park’s research team from the Department of Chemistry at KAIST has successfully developed technology that enables the easy editing and correction of oxygen atoms in furan compounds into nitrogen atoms, directly converting them into pyrrole frameworks, which are widely used in pharmaceuticals. This groundbreaking research was published in the scientific journal Science under the title “Photocatalytic Furan-to-Pyrrole Conversion.”
Many drugs have complex chemical structures, but their efficacy is often determined by a single critical atom. Atoms like oxygen and nitrogen play a central role in enhancing the pharmacological effects of these drugs, particularly against viruses. This phenomenon, known as the “Single Atom Effect,” is crucial in leading-edge drug development, as discovering atoms that maximize drug efficacy is key. However, evaluating the Single Atom Effect has traditionally required multi-step, costly synthesis processes, as it has been difficult to selectively edit single atoms within stable ring structures containing oxygen or nitrogen. Professor Park’s team overcame this challenge by introducing a photocatalyst that uses light energy, acting as a “molecular scissor” that freely cuts and attaches five-membered rings, enabling single-atom editing at room temperature and atmospheric pressure—a world first.
The team discovered a new reaction mechanism in which the excited molecular scissor removes oxygen from furan via single-electron oxidation and then sequentially adds a nitrogen atom. Donghyeon Kim and Jaehyun You, the study’s first authors and candidates in KAIST’s integrated master’s and doctoral program in the Department of Chemistry, emphasized the high versatility of this technique, which utilizes light energy to replace harsh conditions. They noted that the technology enables selective editing, even when applied to complex natural products or pharmaceuticals. Professor Yoonsu Park, the leader of the research team, expressed optimism about the impact of this breakthrough, stating that it will open new doors for building libraries of drug candidates, a key challenge in pharmaceuticals. He hopes that this foundational technology will revolutionize the drug development process.
The significance of this research was acknowledged in the Perspective section of Science, where a peer scientist of prominence outside of the project group provided commentary on the impactful research. The research was supported by the National Research Foundation of Korea’s Creative Research Program, the Cross-Generation Collaborative Lab Project at KAIST, and the POSCO Science Fellowship of the POSCO TJ Park Foundation. This research marks a significant advancement in drug development technology, enabling the selective editing of single atoms within stable ring structures containing oxygen or nitrogen, paving the way for the discovery of novel drug candidates. The ability to easily and rapidly edit key atoms responsible for drug efficacy is a game-changer in the field of pharmaceuticals and has the potential to revolutionize the drug development process.
