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针对结核病治疗的新型 InhA 靶向化合物。

Novel compounds targeting InhA for TB therapy.

机构信息

Department of Biotechnology, Institute of Natural and Applied Sciences (Fen Bilimleri Enstitüsü) Cukurova University, Adana, Turkey.

Department of Biotechnology, Faculty of Industrial Sciences and Technology, University Malaysia Pahang (UMP), Kuantan, Malaysia.

出版信息

Pharmacol Rep. 2018 Apr;70(2):217-226. doi: 10.1016/j.pharep.2017.09.001. Epub 2017 Sep 21.

DOI:10.1016/j.pharep.2017.09.001
PMID:29475004
Abstract

Tuberculosis (TB) is described as lethal disease in the world. Resistant to TB drugs is the main reason to have unfavourable outcomes in the treatment of TB. Therefore, new agents to replace existing drugs are urgently needed. Previous reports suggested that InhA inhibitors, an enoyl-ACP-reductase, might provide auspicious candidates which can be developed into novel antitubercular agents. In this review, we explain the role of InhA in the resistance of isoniazid. Furthermore, five classes of InhA inhibitors, which display novel binding modes and deliver evidence of their prosperous target engagement, have been debated.

摘要

结核病(TB)是世界上致命的疾病。对 TB 药物的耐药性是导致 TB 治疗结果不佳的主要原因。因此,迫切需要新的药物来替代现有的药物。以前的报告表明,烯酰基辅酶 A 还原酶(InhA)抑制剂可能是有希望的候选药物,可以开发成新型抗结核药物。在这篇综述中,我们解释了 InhA 在异烟肼耐药中的作用。此外,还讨论了五类显示出新型结合模式并提供其良好靶标结合证据的 InhA 抑制剂。

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