Efficacy of novel antibacterial compounds targeting histidine kinase YycG protein.
Efficacy of novel antibacterial compounds targeting histidine kinase YycG protein.
复制标题
靶向组氨酸激酶 YycG 蛋白的新型抗菌化合物的功效
DOI：
10.1007/s00253-014-5685-8
复制
发表时间：
2014-07
影响因子：
5
通讯作者：
Qu, Di
中科院分区：
文献类型：
--
作者：
Liu, Huayong;Zhao, Dan;Chang, Jun;Yan, Liang;Zhao, Fuju;Wu, Youcong;Xu, Tao;Gong, Ting;Chen, Li;He, Nianan;Wu, Yang;Han, Shiqing;Qu, Di
关键词：
治疗葡萄球菌生物膜相关感染具有挑战性。基于化合物2靶向表皮葡萄球菌（staphylococcus epidermidisYycG） HK结构域对葡萄球菌具有抗菌和抗膜活性的研究结果，对新合成的6个化合物衍生物进行了抑菌活性评价。化合物2的6个衍生物对YycG的自磷酸化有抑制作用，ic50值在24.2 ~ 71.2 μM之间。该衍生物对浮游生物具有一定的杀菌活性。金黄色葡萄球菌的MIC范围为1.5 ~ 3.1 μM。所有衍生物均对s的6 h和24 h生物膜具有抗菌活性。epidermidis。与原型化合物2相比，它们对Vero细胞的细胞毒性较低，对人红细胞的溶血活性较低。该衍生物对临床耐甲氧西林葡萄球菌分离株具有抑菌活性。YycG抑制剂的结构修饰将有助于发现新的药物来消除生物膜感染和多重耐药葡萄球菌感染。
Treating staphylococcal biofilm-associated infections is challenging. Based on the findings that compound 2 targeting the HK domain ofStaphylococcus epidermidisYycG has bactericidal and antibiofilm activities against staphylococci, six newly synthesized derivatives were evaluated for their antibacterial activities. The six derivatives of compound 2 inhibited autophosphorylation of recombinant YycG′ and the IC50values ranged from 24.2 to 71.2 μM. The derivatives displayed bactericidal activity against planktonicS. epidermidisorStaphylococcus aureusstrains in the MIC range of 1.5–3.1 μM. All the derivatives had antibiofilm activities against the 6- and 24-h biofilms ofS. epidermidis. Compared to the prototype compound 2, they had less cytotoxicity for Vero cells and less hemolytic activity for human erythrocytes. The derivatives showed antibacterial activities against clinical methicillin-resistant staphylococcal isolates. The structural modification of YycG inhibitors will assist the discovery of novel agents to eliminate biofilm infections and multidrug-resistant staphylococcal infections.
登录
查看更多内容
靶向组氨酸激酶 YycG 的噻唑烷酮衍生物可有效对抗浮游和生物膜相关的表皮葡萄球菌
影响因子：
8.2
作者：
Huang, Ren-zheng;Zheng, Li-kang;Qu, Di
通讯作者：
Qu, Di
影响因子：
1.8
作者：
D'Arezzo S;Lanini S;Puro V;Ippolito G;Visca P
通讯作者：
Visca P
影响因子：
3.6
作者：
Bisicchia, Paola;Noone, David;Devine, Kevin M.
通讯作者：
Devine, Kevin M.
DOI：
10.1007/978-1-61779-080-5_34
发表时间：
2011-01-01
期刊：
CANCER CELL CULTURE: METHODS AND PROTOCOLS, SECOND EDITION
影响因子：
--
作者：
Bijnsdorp, Irene V.;Giovannetti, Elisa;Peters, Godefridus J.
通讯作者：
Peters, Godefridus J.
影响因子：
9.4
作者：
Ceri, H;Olson, ME;Buret, A
通讯作者：
Buret, A