With the emergence of multidrug-resistant tuberculosis and extensive drug-resistant tuberculosis strains,there is an urgent need to develop novel drugs for the treatment of tuberculosis.The respiratory chain is a prom...With the emergence of multidrug-resistant tuberculosis and extensive drug-resistant tuberculosis strains,there is an urgent need to develop novel drugs for the treatment of tuberculosis.The respiratory chain is a promising target for the development of newantimycobacterial agents,and a growing number of compounds have been reported and some have entered clinical trials.In this review,we summarize the main features and the electron transfer process of the mycobacterial respiratory chain,and the recent progress in the search for new small molecule inhibitors to rgeting the three main potential targets in the respiratory chain of Mycrobacterium tuberculosis.Our emphasis is on the optimization strategy of QcrB inhibitors and the challenges of developing QcrB inhibitors as antituberculosis drugs due to the alternate bd-type oxidase oxidative compensation pathway are discussed.展开更多
文摘以廉价易得的L-苏氨酸为原料,利用在大肠杆菌中重组表达的苏氨酸脱氨酶和亮氨酸脱氢酶,并偶联基于酮还原酶的NADH再生系统一锅法制备L-2-氨基丁酸。以L-2-氨基丁酸的产率为指标,考察了一锅法酶催化制备L-2-氨基丁酸的最适p H、L-苏氨酸浓度及异丙醇浓度。在最适p H 7.5~8.0,L-苏氨酸浓度50g/L,添加5%的异丙醇及0.5g/L NAD+,分别加入0.6g/L苏氨酸脱氨酶、2g/L亮氨酸脱氢酶及2g/L酮还原酶,反应20h,可实现L-2-氨基丁酸的摩尔产率为99%,产量为43g/L。该结果为L-2-氨基丁酸的制备提供了一种新的思路。
基金financial support from the National Natural Science Foundation of China(No.81922062)Guangdong Provincial Science and Technology Program(No.2018A050506043)and Jinan University。
文摘With the emergence of multidrug-resistant tuberculosis and extensive drug-resistant tuberculosis strains,there is an urgent need to develop novel drugs for the treatment of tuberculosis.The respiratory chain is a promising target for the development of newantimycobacterial agents,and a growing number of compounds have been reported and some have entered clinical trials.In this review,we summarize the main features and the electron transfer process of the mycobacterial respiratory chain,and the recent progress in the search for new small molecule inhibitors to rgeting the three main potential targets in the respiratory chain of Mycrobacterium tuberculosis.Our emphasis is on the optimization strategy of QcrB inhibitors and the challenges of developing QcrB inhibitors as antituberculosis drugs due to the alternate bd-type oxidase oxidative compensation pathway are discussed.
