2010 年 68 巻 9 号 p. 939-950
Bioactive natural products have been used as natural medicines from the beginning of human history. For the last several decades, their utility value has expanded from clinical medicine to basic science, and a number of natural products have been utilized as “bioprobes” for dissecting protein functions and cellular signaling pathways. However, the structural complexity and diversity of these compounds often hamper the necessary mode-of-action analysis and target identification, thereby limiting their utility in chemical biology. Consequently, mode-of-action analysis and target identification of complex natural products still remain a significant challenge in chemical biology and modern drug discovery. Herein, I highlight several examples of our efforts in this area. In the first half of this account, two examples of detailed mode-of-action analysis of complex bioactive natural products are presented. In the second half, a method for immobilizing natural products on solid surfaces is highlighted, and our recent efforts at detecting protein-ligand interactions utilizing this immobilization chemistry are summarized.