含磷丙酮酸脱氢酶系抑制剂的研究进展

丙酮酸脱氢酶系是生物体内重要的氧化还原酶之一,其催化丙酮酸氧化脱羧转化为乙酰辅酶A是生物体内的关键代谢过程,在生物化学研究中具有重要的意义.根据生物化学的理由来进行新药分子生物合理设计的观点,丙酮酸脱氢酶系是一个具有重要意义和值得探索的靶标.研究表明许多有机磷化合物是一类重要的丙酮酸脱氢酶系抑制剂.本文系统介绍了含磷丙酮酸脱氢酶系抑制剂的研究历程和研究动态,并结合本课题组的研究工作对代表性的研究结果和进展进行了总结和评述.

Progresses in research of phosphorus-containing PDHc inhibitors

The pyruvate dehydrogenase complex（PDHc） is one of the most important oxidoreductase in organism.It catalyzes the oxidative decarboxylation of pyruvate to acetyl CoA which is a pivotal process in cellular metabolism and plays a great significance in the biochemical study.So the pyruvate dehydrogenase complex is of interest and worthy of approach from the point of view of agrochemical biorational design.A lot of organophosphorus compounds have been demonstrated as a kind of inhibitor of PDHc.This review focus on the study of history and research progress of phosphorus-containing PDHc inhibitors including the work in our laboratory.The trend on the research and the development of PDHc inhibitors as agrochemical are summarized and discussed.