New inhibitors targeting bacterial RNA polymerase
New inhibitors targeting bacterial RNA polymerase
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DOI：
10.1016/j.tibs.2004.02.005
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发表时间：
2004-04-01
影响因子：
13.8
通讯作者：
Darst, SA
中科院分区：
文献类型：
--
作者：
Darst, SA
细菌RNA聚合酶是抗菌药物的一个已被证实的靶点，因为它被利福平抑制，利福平是一种强效抗生素，是结核病治疗的关键组成部分。细菌RNA聚合酶也是一种分子机器，为尚未开发的小分子抑制剂提供了许多靶标。最近的研究发现了新的抑制剂类别。高通量筛选、药物化学和高分辨率结构研究的进一步应用为抗菌剂的开发带来了巨大的希望。
The bacterial RNA polymerase is a proven target for antimicrobials because it is inhibited by rifampicin, a potent antibiotic that is a key component of tuberculosis therapy. The bacterial RNA polymerase is also a molecular machine that presents numerous targets for small-molecule inhibitors that have not yet been exploited. Recent work has uncovered new classes of inhibitors. Further applications of high-throughput screening, medicinal chemistry and high-resolution structural studies hold great promise for the development of antimicrobials.