siRNA Delivery Using a Cationic-Lipid-Based Highly Selective Human DNA Ligase I Inhibitor,ACS Applied Materials & Interfaces

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siRNA Delivery Using a Cationic-Lipid-Based Highly Selective Human DNA Ligase I Inhibitor
ACS Applied Materials & Interfaces ( IF 8.3 ) Pub Date : 2018-01-02 00:00:00 , DOI: 10.1021/acsami.7b19193
Surendar R. Bathula ₁ , Komal Sharma ₁ , Deependra K. Singh ₂ , Muktapuram P. Reddy ₁ , Pushpa R. Sajja ₁ , Amit L. Deshmukh ₂ , Dibyendu Banerjee ₂

Affiliation

The present article illustrates the serendipitous discovery of a cationic-lipid-based human DNA ligase (hLig) I inhibitor and the development of siRNA delivering, a hLigI-targeted cationic-lipid-based nonviral vector. We have tested a small in-house library of structurally similar cationic lipo-anisamides for antiligase activity, and amongst tested, N-dodecyl-N-(2-(4-methoxybenzamido)ethyl)-N-methyldodecan-1-ammonium iodide (C12M) selectively and efficiently inhibited the enzyme activity of hLigI, compared to other human ligases (hLigIIIβ and hLigIV/XRCC4) and bacterial T4 DNA ligase. Furthermore, upon hydration with equimolar cholesterol, C12M produced antiligase cationic liposomes, which transfected survivin siRNA and showed significant inhibition of tumor growth.

中文翻译：

使用基于阳离子脂质的高选择性人类DNA连接酶I抑制剂的siRNA传递。

本文阐述了基于阳离子脂质的人DNA连接酶（hLig）I抑制剂的偶然发现以及基于hLigI靶向的基于阳离子脂质的非病毒载体的siRNA传递的发展。我们已经测试了一个内部结构相似的阳离子脂类茴香酰胺的小型内部文库的抗连接酶活性，其中包括N-十二烷基-N-（2-（4-甲氧基苯甲酰胺基）乙基）-N-甲基十二烷基-1-碘化铵（C12M）选择性地且有效地抑制hLigI的酶活性，相对于其他人的连接酶（hLigIIIβ和hLigIV / XRCC4）和细菌T4 DNA连接酶。此外，与等摩尔胆固醇水合后，C12M 产生抗连接酶阳离子脂质体，转染survivin siRNA并显示出对肿瘤生长的显着抑制作用。

更新日期：2018-01-02

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