来自天然产物的靶向结核分枝杆菌ClpC1的抗结核先导分子。
Anti-tuberculosis lead molecules from natural products targeting Mycobacterium tuberculosis ClpC1.
作者信息
Lee Hanki, Suh Joo-Won
机构信息
Center for Nutraceutical and Pharmaceutical Materials, Myongji University, Yongin, Gyeonggi-do, 17058, South Korea.
Division of Biosciences and Bioinformatics, College of Natural Science, Myongji University, Yongin, Gyeonggi-do, 17058, South Korea.
出版信息
J Ind Microbiol Biotechnol. 2016 Mar;43(2-3):205-12. doi: 10.1007/s10295-015-1709-3. Epub 2015 Nov 19.
Tuberculosis (TB) is a serious and potentially fatal disease caused by Mycobacterium tuberculosis (M. tb). The occurrence of multidrug-resistant (MDR) and extensively drug-resistant (XDR) M. tb is a significant public health concern because most of the anti-TB drugs that have been in use for over 40 years are no longer effective for the treatment of these infections. Recently, new anti-TB lead compounds such as cyclomarin A, lassomycin, and ecumicin, which are cyclic peptides from actinomycetes, have shown potent anti-TB activity against MDR and XDR M. tb as well as drug-susceptible M. tb in vitro. The target molecule of these antibiotics is ClpC1, a protein that is essential for the growth of M. tb. In this review, we introduce the three anti-TB lead compounds as potential anti-TB therapeutic agents targeting ClpC1 and compare them with the existing anti-TB drugs approved by the US Food and Drug Administration.
结核病（TB）是由结核分枝杆菌（M. tb）引起的一种严重且可能致命的疾病。耐多药（MDR）和广泛耐药（XDR）结核分枝杆菌的出现是一个重大的公共卫生问题，因为已使用40多年的大多数抗结核药物对这些感染的治疗不再有效。最近，新的抗结核先导化合物，如来自放线菌的环孢菌素A、拉索霉素和依库米星等环肽，在体外对耐多药和广泛耐药结核分枝杆菌以及药物敏感结核分枝杆菌均显示出强大的抗结核活性。这些抗生素的靶分子是ClpC1，一种对结核分枝杆菌生长至关重要的蛋白质。在本综述中，我们介绍这三种作为靶向ClpC1的潜在抗结核治疗剂的抗结核先导化合物，并将它们与美国食品药品监督管理局批准的现有抗结核药物进行比较。
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