一种三官能团自毁间隔基可通过两种非连续的酶切实现药物释放。
A trifunctional self-immolative spacer enables drug release with two non-sequential enzymatic cleavages.
机构信息
Università degli Studi di Milano, Dipartimento di Chimica, via C. Golgi, 19, Milan, I-20133, Italy.
Fondazione IRCCS Istituto Nazionale dei Tumori, Molecular Pharmacology Unit, Department of Applied Research and Technological Development, via Amadeo 42, Milan, 20133, Italy.
出版信息
Chem Commun (Camb). 2021 Aug 5;57(63):7778-7781. doi: 10.1039/d1cc02895b.
Cyclative cleavage of an amine-carbamate self-immolative spacer to deliver a hydroxyl cargo was inhibited by spacer derivatisation with a phosphate monoester handle. This trifunctional spacer was installed in a model anticancer prodrug that showed fast drug release only when incubated with both a protease and a phosphatase enzyme.
通过将带有磷酸单酯接头的间隔臂衍生化，抑制了胺基碳酸酯自毁间隔臂的环化裂解以递送羟基货物。该三功能间隔臂被安装在一种模型抗癌前药中，只有在与蛋白酶和磷酸酶同时孵育时，该前药才显示出快速释放药物的特性。
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