ABSTRACT

Natural product research was once limited to dening the chemistry of small molecules and looking for novel structural scaffolds. Today, natural products have successfully integrated the biology of small molecules-dening the biological activity, unraveling the cellular target, and deciphering the mechanism of action in cellular systems. Both the chemistry and biology of small molecules from natural sources helped shape the role of natural products in drug discovery. Nature has been regarded as one of the most successful producers of new small-molecule therapeutics, primarily due to the chemodiversity and potent biological activity of natural products. Aside from drug discovery, these small molecules also serve as excellent molecular probes due to the high afnity for their cellular targets arising from optimization through evolution. Natural products are recognized to be an integral part of chemical biology in dening the structure and function of proteins and signaling networks.