Persson Tobias, Givskov Michael, Nielsen John
Department of Natural Sciences, Bioorganic Chemistry Section, The Royal Danish Veterinary and Agricultural University, DK-1871 Frederiksberg C, Denmark.
Curr Med Chem. 2005;12(26):3103-15. doi: 10.2174/092986705774933425.
Quorum sensing (QS) systems comprise a new therapeutic target potentially substitutive or complementary to traditional antibiotic treatment of chronic diseases. One route to disrupt the previously established interrelationship between pathogenesis and QS is by blocking the dual functioning signal/receptor transcriptional regulator in some clinically relevant Gram-negative bacteria. The present review contains all reported compound types that are currently known to inhibit the QS transcriptional regulator in Gram-negative bacteria. These compounds are sub-divided into two main groups, one comprising structural analogs of the native signaling molecules and the other compounds lacking structural resemblance. Biological activity is rationalized on the basis of structure-activity relationships and structural insight into the target protein.
群体感应（QS）系统构成了一个新的治疗靶点，可能替代或补充传统抗生素对慢性疾病的治疗。破坏先前建立的发病机制与群体感应之间相互关系的一种途径是阻断某些临床相关革兰氏阴性菌中的双功能信号/受体转录调节因子。本综述涵盖了目前已知的所有可抑制革兰氏阴性菌中群体感应转录调节因子的化合物类型。这些化合物分为两大类，一类是天然信号分子的结构类似物，另一类是缺乏结构相似性的化合物。基于构效关系和对靶蛋白的结构洞察，对生物活性进行了合理化分析。
