KCS

After the completion of the human genome project, it is estimated that there are up to 10,000 disease related genes in the human genome. The goal in post-genomic era would be to understand and control the functions of each gene. Therefore, there is an urgent need to develop molecules that can modulate the functions of these disease-related proteins. Such molecules could not only serve as invaluable probes to delineate the protein functions, but also be further developed as therapeutic candidates. However, it is very challenging to deal with overwhelming numbers of target proteins to discover molecules targeting each protein. Furthermore, many proteins (e.g., those that are involved in protein-protein interactions) are not readily targeted by typical small drug-like molecules. Here I will present our chemical approaches to discover such molecules capable of modulating proteins functions, which include the development of new chemical space (suitable for currently undruggable targets), new methods for modulating cellular proteins, and ultra high-throughput screening methods for facilitating rapid identification of protein ligands.