Villain-Guillot Philippe, Bastide Lionel, Gualtieri Maxime, Leonetti Jean-Paul
CNRS UMR 5236, UM1 UM2, Centre d'études d'agents pathogènes et Biotechnologies our la Santé, Av Charles Flahault, 34093 Montpellier, France.
Drug Discov Today. 2007 Mar;12(5-6):200-8. doi: 10.1016/j.drudis.2007.01.005. Epub 2007 Feb 5.
The bacterial RNA polymerase (RNAP) is an essential enzyme that is responsible for making RNA from a DNA template and is targeted by several antibiotics. Rifampicin was the first of such antibiotics to be described and is one of the most efficient anti-tuberculosis drugs in use. In the past five years, structural studies of bacterial RNAP and the resolution of several complexes of drugs bound to RNAP subunits have revealed molecular details of the drug-binding sites and the mechanism of drug action. This knowledge opens avenues for the development of antibiotics. Here these drugs are reviewed, together with their mechanisms and their potential interest for therapeutic applications.
细菌RNA聚合酶(RNAP)是一种必需的酶,负责以DNA模板合成RNA,并且是几种抗生素的作用靶点。利福平是最早被描述的此类抗生素之一,也是目前使用的最有效的抗结核药物之一。在过去五年中,对细菌RNAP的结构研究以及几种与RNAP亚基结合的药物复合物的解析,揭示了药物结合位点的分子细节和药物作用机制。这些知识为抗生素的开发开辟了道路。在此对这些药物及其作用机制以及它们在治疗应用中的潜在价值进行综述。