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Diverted Total Synthesis of Carolacton-Inspired Analogs Yields Three Distinct Phenotypes in Streptococcus mutans Biofilms
Journal of the American Chemical Society ( IF 14.4 ) Pub Date : 2017-05-13 00:00:00 , DOI: 10.1021/jacs.7b03879
Amy E. Solinski 1 , Alexander B. Koval 1 , Richard S. Brzozowski 1 , Kelly R. Morrison 1 , Americo J. Fraboni 1 , Carrie E. Carson 1 , Anisa R. Eshraghi 1 , Guangfeng Zhou 1 , Robert G. Quivey 2 , Vincent A. Voelz 1 , Bettina A. Buttaro 3 , William M. Wuest 1
Affiliation  

The oral microbiome is a dynamic environment inhabited by both commensals and pathogens. Among these is Streptococcus mutans, the causative agent of dental caries, the most prevalent childhood disease. Carolacton has remarkably specific activity against S. mutans, causing acid-mediated cell death during biofilm formation; however, its complex structure limits its utility. Herein, we report the diverted total synthesis and biological evaluation of a rationally designed library of simplified analogs that unveiled three unique biofilm phenotypes further validating the role of natural product synthesis in the discovery of new biological phenomena.

中文翻译:

转移总合成的灵感来自加罗顿的类似物在变形链球菌生物膜中产生三种不同的表型。

口腔微生物组是一个由共生菌和病原体共同居住的动态环境。其中包括变形链球菌,龋齿的致病因子,龋齿是儿童中最普遍的疾病。Carolacton对变形链球菌具有显着的特异性活性,在生物膜形成过程中引起酸介导的细胞死亡。但是,其复杂的结构限制了其实用性。在这里,我们报告了合理设计的简化类似物库的转向总合成和生物学评估,该库揭示了三种独特的生物膜表型,进一步验证了天然产物合成在发现新的生物现象中的作用。
更新日期:2017-05-18
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