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可光切换的甘氨基基向Pseudomonas aeruginosa LecA的目标

Yu Fan¹, Ahmed El Rhaz², Stéphane Maisonneuve¹

¹Université Paris-Saclay, ENS Paris-Saclay, Institut d'Alembert, CNRS, Photophysique et Photochimie Supramoléculaires et Macromoléculaires, 91190, Gif-sur-Yvette, France.

Beilstein journal of organic chemistry

|July 9, 2024

概括

研究人员开发了光敏感的甘氨基干细胞来控制像LecA这样的细菌学菌素,为抗生素耐药性感染提供了一种新的策略. 这些可光切换的分子表现出强烈的结合亲和力,为新型抗感染疗法铺平了道路.

科学领域:

微生物学微生物学
药用化学医学化学
生物物理化学生物物理化学

背景情况:

由* Pseudomonas aeruginosa*形成的生物膜有助于抗菌素耐药性和感染.
可溶性莱克LecA和LecB对于生物膜发育和肺部感染至关重要.
细菌莱克是开发新型抗生素节约抗感染剂的有希望的目标.

研究的目的:

设计和合成可光切换的甘油聚合物,准*Pseudomonas aeruginosa*的莱丁LecA.
评估这些新型配体的结合亲和力和热力学特性.
为了探索潜在的治疗应用,光控制调节莱克活性.

主要方法:

合成*O*-和*S*-Galactosyl亚博烯衍生物.
使用异热定位热量计 (ITC) 评估结合亲和力.
对连接体结合的热力学贡献 (和) 的分析.

主要成果:

合成的单价糖联体体具有出色的光物理性质.
这些配体对LecA具有强烈的结合亲和力,在微分子范围内的解离常数 (*K*_d).
热力学分析揭示了*E*-和*Z*-阿佐异构体之间明显的-贡献,影响了整体亲和力.

结论:

可光切换的甘油聚合物向细菌学菌素是可行的,并显示出显著的结合亲和力.
该研究验证了光控制调节莱克活性的概念证明.
剖析结合的热力学可以为设计改进的,可光激活的乳抑制剂提供见解.

关键词:

碳水化合物碳水化合物糖酸阿本酸盐的含量是多少莱克A是一种可光切换的带是可以光切换的.

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