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一个基于氨酸光化学的近IR脱策略

Alexander P Gorka¹, Roger R Nani, Jianjian Zhu

¹Chemical Biology Laboratory, National Cancer Institute , 376 Boyles Street, Frederick, Maryland 21702, United States.

Journal of the American Chemical Society

|September 12, 2014

概括

研究人员开发了一种使用近红外光来控制药物输送的新型光方法. 这种技术能够精确地在空间和时间上释放小分子,增强基础研究和治疗应用.

科学领域:

化学生物学化学生物学
摄影化学的使用.
药物输送系统药物输送系统

背景情况:

靠近红外线 (NIR) 光激活的光组为生物研究和药物输送提供了先进的控制.
开发高效和生物相容的NIR激活光系统对于生物系统中精确的分子操纵至关重要.

研究的目的:

为小分子开发一种新的NIR光启动的脱反应序列.
证明这种系统对控制生物过程的有用性,包括细胞活力和基因表达.

主要方法:

合成C4'-二甲基胺替代的氨酸氨酸素作为光支架.
开发了一种连续的解锁机制,涉及氨基释放和分子内循环.
在基于细胞的测试中应用脱系统以抑制细胞活力和控制基因表达.

主要成果:

证明了一种新的NIR光启动的脱反应,该反应基于氨酸甲.
通过使用低强度690nm光来展示与生物环境的脱兼容性.
通过光依赖释放4-基环,成功抑制细胞活力和控制基因表达.

结论:

建立了一种化学基础,用于以NIR光介导的含小分子的脱.
验证了生物系统中分子传递的空间和时间控制潜力.
这项技术使得使用生物相容,穿透组织的NIR光来实现向的小分子输送.

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