细菌RNA聚合酶抑制剂的研究进展

Advances in the development of bacterial RNA polymerase inhibitors

细菌RNA聚合酶(RNA polymerase,RNAP)在细菌的生命周期中发挥重要的作用,是催化转录合成RNA的关键酶。RNAP抑制剂可通过作用于RNAP的活性中心及其附近,阻止细菌的RNA链的延伸从而抑制RNAP的活性。近年来,RNAP已成为筛选高效广谱抗菌药物的热门靶标,新型RNAP抑制剂的研究取得了较大的进展,已获得多种结构类型的新型RNAP抑制剂。本文就近年来报道的RNAP抑制剂进行综述。

Bacterial RNA polymerase(RNAP)plays an important role in the life cycle of bacteria,which is the key enzyme of catalytic synthesis of RNA transcription.RNAP inhibitors act on the enzyme active center and its nearby sites and prevent bacteria RNA chain extension to inhibit the activity of RNAP.In recent years,RNAP has become one of the most popular targets for screening new antibacterial agents with broad-spectrum and highpotency,and great progress has been made in the research on RNAP inhibitors with their various structural types having been obtained.The natural and synthetic RNAP inhibitors reported in recent years were introduced in this article.