119th General Meeting of the KCS

Type Award Lecture in Division
Area Current Trends in Organic Chemistry Ⅰ: Methodology and Application
Room No. 302호
Time THU 13:30-:
Code ORGN1-1
Subject Design, Synthesis, and Biological Application of Proteomimetics as Protein-Protein Interaction Inhibitors
Authors 임현석
POSTECH 화학과, Korea
Abstract The majority of drugs on the market today target proteins with well-defined small-molecule binding sites, including enzymes. However, some of the most devastating diseases are caused by proteins that do not possess these natural binding sites, such as those involved in protein-protein interactions associated with many cancers. Synthetic molecules capable of inhibiting disease-related protein-protein interactions are thus valuable research tools to investigate molecular functions of target proteins and further could be developed as novel therapeutic candidates. However, discovering such inhibitors is a daunting task due largely to the relatively large and flat protein interfaces involved in protein-protein interactions. In general, typical drug-like small molecules may not be suitable to effectively cover such extended protein contact areas. As such, there is an urgent need for the development of different types of molecules to target protein interfaces. In addition, the shortage of convenient high-throughput screening (HTS) methods is another important reason that makes the identification of such inhibitors so challenging. Here I will present our design and synthesis of novel chemical entities called proteomimetics that are able to mimic protein surface structure and function, allowing them to serve as an excellent source of protein ligands. Moreover, I will also introduce our recent development of simple and efficient HTS methods that enables to facilitate the discovery of chemical inhibitors of many disease-causing protein-protein interactions.
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