分枝杆菌膜蛋白3抑制剂的研究进展

发布时间：2018-06-05 21:23

本文选题：分枝杆菌膜蛋白 + 结核分枝杆菌　；参考：《药学学报》2017年09期

【摘要】：分枝杆菌膜蛋白3(mycobacterial membrane protein large 3,Mmp L3)属于抗瘤细胞分裂(RND)蛋白超家族,它主要参与结核分枝杆菌中海藻糖单霉菌酸酯的转运过程,对Mmp L3的抑制可以影响结核分枝杆菌细胞壁的合成。近年来,通过表型筛选已发现并确证了7类不同化学骨架的Mmp L3抑制剂,拟用于耐药结核病的治疗。本文将简要论述这几类Mmp L3抑制剂及其构效关系,介绍靶标确证的方法,并进一步探讨Mmp L3抑制剂的作用机制。
[Abstract]:Mycobacterium membrane protein 3(mycobacterial membrane protein large _ 3 / MMP _ L _ 3 belongs to the superfamily of anti-tumor cell division (RND) protein, which is mainly involved in the transport of mycobacterium alginate monophosphate in Mycobacterium tuberculosis, and the inhibition of MMP L _ 3 can affect the synthesis of cell wall of Mycobacterium tuberculosis. In recent years, seven kinds of MMP L3 inhibitors with different chemical cytoskeleton have been identified and confirmed by phenotypic screening, which can be used in the treatment of drug-resistant tuberculosis. This paper briefly discusses these MMP L3 inhibitors and their structure-activity relationships, introduces the methods of target identification, and further discusses the mechanism of MMP L3 inhibitors.
【作者单位】：中国医学科学院北京协和医学院药物研究所活性物质发现与适药化研究北京市重点实验室;
【基金】：国家科技重大专项“重大新药创制”子课题2015ZX09102007“抗耐药结核新药TBI-001的临床前研究”
【分类号】：R978

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