As a pioneer in drug development, new technology that enables easy and rapid editing of key atoms responsible for drug efficacy has been considered a fundamental and “dream” technology, revolutionizing the discovery process of potential drug candidates . KAIST researchers have become the first in the world to successfully develop a single-atom editing technology that maximizes drug efficacy.
On October 8, KAIST (represented by President Kwang-Hyung Lee) announced that Professor Yoonsu Park’s research team from the Department of Chemistry successfully developed a technology that allows the oxygen atoms of furan compounds to be easily edited and corrected. into nitrogen atoms, converting them directly into pyrrole structures, which are widely used in pharmaceuticals.
This research was published in the scientific journal. Science on October 3 under the title “Photocatalytic conversion of furan to pyrrole.”
Many drugs have complex chemical structures, but their effectiveness is often determined by a single critical atom. Atoms such as oxygen and nitrogen play a central role in enhancing the pharmacological effects of these drugs, particularly against viruses.
This phenomenon, in which the introduction of specific atoms into a drug molecule dramatically affects its effectiveness, is known as the “single atom effect.” In cutting-edge drug development, the key is to discover atoms that maximize drug efficacy.
However, evaluation of the single-atom effect has traditionally required expensive, multi-step synthesis processes, as it has been difficult to selectively edit individual atoms within stable oxygen- or nitrogen-containing ring structures.
Professor Park’s team overcame this challenge by introducing a photocatalyst that uses light energy. They developed a photocatalyst that acts like a “molecular scissors,” freely cutting and joining 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 excited molecular scissors remove oxygen from furan through single-electron oxidation and then sequentially add a nitrogen atom.
Donghyeon Kim and Jaehyun You, the first authors of the study and candidates in KAIST’s integrated master’s and doctoral program in the Department of Chemistry, explained that this technique offers great versatility by using light energy to replace harsh conditions. They further noted that the technology allows for selective editing, even when applied to complex natural or pharmaceutical products. Professor Yoonsu Park, who led the research, commented: “This breakthrough, which enables selective editing of five-membered organic ring structures, will open new doors for the construction of candidate drug libraries, a key challenge in the pharmaceutical sector. “I hope this will be instrumental. The technology will be used to revolutionize the drug development process.”
The importance of this research was highlighted in the Science Perspective section, a feature where a leading scientist outside the project group provides commentary on impactful research.
This research was supported by the Creative Research Program of the National Research Foundation of Korea, the Intergenerational Collaborative Laboratory Project at KAIST, and the POSCO TJ Park Foundation POSCO Scientific Grant.