Chemical Biology/ Chemical Genetics/ Chemical Genomics: Importance of Chemical Library

A new field of science, chemical biology/ chemical genetics/ chemical genomics (cb/cg/cg) has emerged since the late 1990's, especially in the United States. The NIH Roadmap agenda, Molecular Libraries Screening Center Network (MLSCN), became a drive force to push cb/cg/cg forward. Cb/cg/cg studies consist of three methodologies, chemical libraries with small molecules, high-throughput screenings, and computational databases. In this review, we focus on the importance of chemical libraries. Natural products-originated chemical libraries or their synthesized related compounds-derived chemical libraries have long contributed to human health sciences in mainly pharmaceutical industries. The reason why natural products have been of interest is that they consist of diverse and complex chemical compounds. This character makes natural compounds important as the seed of future medicine. Currently, pharmaceutical industry-based chemical biology using biology-oriented chemical libraries has spun off into the cb/cg/cg studies for basic biology in non-profit scientific organizations and a variety of developments have resulted from the use of chemical libraries with natural products. To overcome the diversity and complexity of nature-originated chemical compounds, a new concept of synthesizing small chemical compounds, Diversity-Oriented Synthesis (DOS), has been established by Harvard chemist, Stuart Schreiber in late 1990's. Using split-pool synthesizing methodology, small molecules produced by DOS make it possible for us to obtain compounds that span a wide chemical space. Here, we discuss cb/cg/cg studies applied to signal transduction, stem cell differentiation and small G-protein researches. All of these studies are conducted not only using biology-oriented libraries but also DOS-oriented libraries. Although cb/cg/cg is a relatively young science that aims the post-genome era sciences, it must bridge chemistry and biology not only in the academia but also in pharmaceutical industries.