乙酰乳酸合成酶及其抑制剂研究新进展

乙酰乳酸合成酶(AHAS)是支链氨基酸生物合成途径中的一个关键酶,是绿色除草剂的重要作用靶标。由于此生物合成过程只存在于植物和微生物体内,因此该类抑制剂对哺乳动物具有生物安全性。近年来,随着AHAS三维结构的阐明,人们不仅深入了解了已有抑制剂的作用机制,并且依此设计开发了一些新型的抑制剂,拓展了其在抑菌活性方面的生物学功能。文章对近年来AHAS及其抑制剂的最新研究进展进行了综述,重点就AHAS的酶学特征、结构特征及结合方式,以AHAS为靶标的新颖除草活性化合物的设计开发以及AHAS抑制剂的抗菌生物活性研究进展等问题详细进行了总结,以期为设计开发靶向AHAS的新型除草剂或抗菌药物提供参考。

Recent progress on acetohydroxyacid synthase and its inhibitors

Acetohydroxyacid synthase (AHAS) is a key enzyme involved in the biosynthesis pathway of branched-chain amino acids, and it is an important target for green herbicides. This enzyme only exists in plants and microbes, therefore its inhibitors are biologically safe to mammals. With the recent elucidation of three dimensional AHAS structures, detailed understanding on the inhibition mechanism of current inhibitors has been achieved, and novel AHAS inhibitors have been designed and discovered. Moreover, AHAS inhibitors have been investigated their new biological function as antimicrobial agents. This review summarizes the progress on AHAS and its inhibitors within recent years, in order to provide useful information for the development of novel herbicides or antibiotics targeting AHAS.