New target for inhibition of bacterial RNA polymerase: 'switch region'.
New target for inhibition of bacterial RNA polymerase: 'switch region'.
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DOI：
10.1016/j.mib.2011.07.030
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发表时间：
2011-10
影响因子：
5.4
通讯作者：
Ebright, Richard H.
中科院分区：
文献类型：
--
作者：
Srivastava, Aashish;Talaue, Meliza;Liu, Shuang;Degen, David;Ebright, Richard Y.;Sineva, Elena;Chakraborty, Anirban;Druzhinin, Sergey Y.;Chatterjee, Sujoy;Mukhopadhyay, Jayanta;Ebright, Yon W.;Zozula, Alex;Shen, Juan;Sengupta, Sonali;Niedfeldt, Rui Rong;Xin, Cai;Kaneko, Takushi;Irschik, Herbert;Jansen, Rolf;Donadio, Stefano;Connell, Nancy;Ebright, Richard H.
一个新的药物靶点——“开关区”——已经在细菌RNA聚合酶（RNAP）中被发现，RNAP是一种介导细菌RNA合成的酶。新靶点作为抑制细菌RNA合成和杀死细菌的化合物的结合位点。由于新靶标存在于大多数细菌物种中，与新靶标结合的化合物对广泛的细菌物种具有活性。由于新靶点不同于其他抗菌剂的靶点，与新靶点结合的化合物不会与其他抗菌剂产生交叉耐药。已经确定了四种通过新靶点起作用的抗生素：myxopyronin， corallopyronin， ritpostatin和lipiarmycin。本文综述了开关区、开关区抑制剂及其对抗菌药物发现的启示。
A new drug target-- the "switch region"--has been identified within bacterial RNA polymerase (RNAP), the enzyme that mediates bacterial RNA synthesis. The new target serves as the binding site for compounds that inhibit bacterial RNA synthesis and kill bacteria. Since the new target is present in most bacterial species, compounds that bind to the new target are active against a broad spectrum of bacterial species. Since the new target is different from targets of other antibacterial agents, compounds that bind to the new target are not cross-resistant with other antibacterial agents. Four antibiotocs that function through the new target have been identified: myxopyronin, corallopyronin, ripostatin, and lipiarmycin. This review summarizes the switch region, switch-region inhibitors, and implications for antibacterial drug discovery.
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