【摘要】 细菌RNA聚合酶(RNA polymerase,RNAP)是筛选高效广谱抗菌药物的重要靶点之一,RNAP抑制剂通过影响细菌RNA的合成达到抗菌功效。本文综述了黏细菌产生的myxopyronins、corallopyronins、sorangicins、ripostatins和etnangiens五种RNAP抑制剂的化学结构和作用机理。其中,sorangicins和利福霉素的作用机制基本相同,能够在RNAP-启动子转录复合体形成后抑制转录的起始;myxopyronins、corallopyronins和ripostatins的作用机制相似,可破坏RNA聚合酶和DNA分子上的启动子结合;etnangiens与corallopyronins均含有较长的侧链结构,作用机理可能相似。目前,黏细菌产生的RNA聚合酶抑制剂已成为开发广谱抗菌药物的一类重要候选化合物。更多还原

【Abstract】 Bacterial RNA Polymerase(RNAP) is always selected as one of the primary target for screening new antibacterial agent with broad-spectrum and high-potency.RNAP Inhibitor restrains the synthesis of nucleic acid of bacteria,thereby disturbs their growth and metabolism,resulting in antibacterial effect.Myxobacteria are capable of producing large numbers of bioactive compounds with unique structures and diverse functions,some of which possess antibacterial bioactivity.This review summarized the chemical structures and biological activity mechanisms of five RNAP inhibitors produced by myxobacteria,including myxopyronins,corallopyronins,sorangicins,ripostatins and etnangiens.Sorangicins inhibits the initiation of eubacterial RNA chain after the RNAP-promoter closed complex to take shape.Myxopyronins,corallopyronins and ripostatins have the same mechanism that blocks RNAP attachment to DNA promoter.Both etnangiens and corallopyronins contain a long side chain and may share a similar action mechanism.In general,it is expected that the myxobacterial RNAP inhibitors become attractive candidates for development of broad-spectrum antibacterial therapeutic agents.更多还原