New method for identifying target molecules of bioactive compounds

点击翻译按钮获取中文摘要

Identification of the target molecule of a bioactive compound is most important for clarifying the mode of action of the compound. The target molecule can afford a clue to investigate the unknown biological phenomenon concerning the bioactive compound at the molecular level. In this study, we attempted to develop a novel method for identifying the target molecule using a dimer probe. Mycotoxin production inhibitors and allosamidin, a chitinase inhibitor, were used as model bioactive compounds. A dimer of precocene II, specific inhibitor of trichothecenes, was prepared based on the structure-activity relationship work, but no dimer with inhibitory activity was obtained. Therefore, we tried to investigate its target molecule using click chemistry and magnetic affinity-beads methods, which are recently developed, by comparing the methods with conventional photoaffinity probe method, and we have gotten a candidate protein as the target molecule. Preparation of allosamidin dimers is ill in progress because it is difficult to connect two allosamidin molecules at desirable positions.