The Future of Pharmaceuticals: Single-atom Editing Technology by KAIST

By Beth He

Many drugs have complex structures designed to treat, prevent, and ease symptoms and viruses, yet their efficacy is often solely determined by a single atom. This phenomenon is known as the ‘Single Atom Effect,’ and is particularly evident in atoms such as oxygen and nitrogen. A drug’s efficacy is defined as “its ability to produce the maximal response possible for a particular biological system.” Scientists and medical researchers have long aimed to enhance drugs’ efficacies as it allows for a greater benefit to the user with the same amount and type of drug. Specifically, single-atom editing targets the atom that primarily determines a drug’s efficacy to optimize its potential effect.

On October 8th, 2024, the Korea Advanced Institute of Science and Technology (KAIST) announced that Professor Yoonsu Park’s research team from the Department of Chemistry had successfully developed a technology capable of editing oxygen atoms in furan compounds into nitrogen atoms. Furans are compounds containing a five-membered aromatic ring with four carbon atoms and one oxygen atom, often used in the manufacture of pharmaceuticals. After the editing, the compounds are then directly converted into pyrrole frameworks. Pyrrole frameworks are structures with pyrrole, a five-membered heterocyclic compound consisting of four carbon atoms and one nitrogen atom. By transforming oxygen-containing furans into nitrogen-containing pyrroles, this technology enables scientists to modify drug structures in ways that were previously unattainable.

To do this, Professor Park’s team introduced a photocatalyst that harnesses light energy to bring the material to a higher energy level and cause previously impossible reactions to occur. In this case, the photocatalyst they developed acts as a “molecular scissor” to freely cut the furan rings and make the desired edits. This molecular scissor, excited from the light energy, undergoes a newly discovered reaction mechanism where it removes oxygen through single-electron oxidation and then adds a nitrogen atom.

Traditional single-atom editing methods often required multiple steps, incurred high costs, and struggled to readily edit stable ring structures containing oxygen and nitrogen. Now, this new technology can not only selectively edit such complex compounds, but it also operates at room temperature and atmospheric pressure due its reliance on light energy. With this revolutionary advancement, scientists have a powerful tool to refine drug compounds, opening the door to more adaptable treatments for a variety of diseases. The ability to edit single atoms with such specificity and under such mild conditions allows drug efficacy to be more closely tailored to individual needs, ultimately minimizing side effects and improving patient outcomes.

Works Cited

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National Center for Biotechnology Information. "PubChem Compound Summary for CID 8029, Furan" PubChem, https://pubchem.ncbi.nlm.nih.gov/compound/Furan. Accessed 7 November, 2024.

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