Selective Mycobacterium tuberculosis Shikimate Kinase Inhibitors as Potential Antibacterials
Selective Mycobacterium tuberculosis Shikimate Kinase Inhibitors as Potential Antibacterials
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DOI：
10.4137/pmc.s13212
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发表时间：
2015-01-01
期刊：
影响因子：
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通讯作者：
Calderon, Angela I.
中科院分区：
文献类型：
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作者：
Gordon, Sara;Simithy, Johayra;Calderon, Angela I.
由于结核病(TB)的持续存在以及这种疾病的多药耐药和广泛耐药(XDR)形式的出现，开发新的抗结核药物至关重要。开发莽草酸途径中的莽草酸激酶(SK)抑制剂将为抗结核药物提供一个选择性靶点。许多研究已经使用电子计算机技术来识别预期与SK相互作用并抑制SK的化合物。在更有限的范围内，已经用纯化的酶通过体外方法评估了SK的抑制作用。目前，文献中还没有关于结核分枝杆菌莽草酸激酶(MtSK)抑制剂体内活性的数据。本文就SK抑制剂的发现和评价进展作一综述，并着重介绍新的抗结核药物的开发。
Owing to the persistence of tuberculosis (TB) as well as the emergence of multidrug-resistant and extensively drug-resistant (XDR) forms of the disease, the development of new antitubercular drugs is crucial. Developing inhibitors of shikimate kinase (SK) in the shikimate pathway will provide a selective target for antitubercular agents. Many studies have used in silico technology to identify compounds that are anticipated to interact with and inhibit SK. To a much more limited extent, SK inhibition has been evaluated by in vitro methods with purified enzyme. Currently, there are no data on in vivo activity of Mycobacterium tuberculosis shikimate kinase (MtSK) inhibitors available in the literature. In this review, we present a summary of the progress of SK inhibitor discovery and evaluation with particular attention toward development of new antitubercular agents.