Chenical biology research using diketopiperazine-based anti-microtubule agent.

点击翻译按钮获取中文摘要

In order to understand the precise binding site of diketopiperadine-based anti-microtubule agent 'plinabulin' on tubulin, we designed and synthesized biotin-tagged plinabulin derivatives as chemical probes. Since these derivatives all showed a significant binding ability to tubulin and cytotoxicity, we performed tubulin photoaffinity labeling study. These results suggested that plinabulin derivatives may bind at the boundary region formed between the α-and β-tubulin subunits around the colchicine binding site, but not inside the site, to effectively disrupt the interaction between the two tubulin subunits, thereby producing microtubule depolymerization.