DNA-Templated organic synthesis (DTS): A novel approach to the discovery of functional small molecules based on nature's evolutionary principles

DNA-templated organic synthesis (DTS) has recently emerged as a general approach to translate DNA sequences into DNA-linked synthetic small molecules. DNA templates not only direct chemistries to construct small molecules but also serve as amplifiable encodings used to identify the chemical structures of the small molecules. Therefore, through DTS, synthetic small molecules can now be subjected to in vitro selection methods for the discovery of novel functional molecules. In this account, we describe the early efforts conducted in the Liu Laboratory to develop key technologies in DTS and new findings toward exploring the potential of a selection-based approach to the discovery of functional small molecules.