用于检测体内蛋白水解活性的自组装金纳米粒子分子探针。
Self-assembled gold nanoparticle molecular probes for detecting proteolytic activity in vivo.
机构信息
Harvard-MIT Division of Health Sciences and Technology, Cambridge, Massachusetts 02139, USA.
出版信息
ACS Nano. 2010 Mar 23;4(3):1511-20. doi: 10.1021/nn9017334.
Abstract
Target-activatable fluorogenic probes based on gold nanoparticles (AuNPs) functionalized with self-assembled heterogeneous monolayers of dye-labeled peptides and poly(ethylene glycol) have been developed to visualize proteolytic activity in vivo. A one-step synthesis strategy that allows simple generation of surface-defined AuNP probe libraries is presented as a means of tailoring and evaluating probe characteristics for maximal fluorescence enhancement after protease activation. Optimal AuNP probes targeted to trypsin and urokinase-type plasminogen activator required the incorporation of a dark quencher to achieve 5- to 8-fold signal amplification. These probes exhibited extended circulation time in vivo and high image contrast in a mouse tumor model.
摘要
基于金纳米粒子 (AuNPs) 的靶向激活荧光探针，通过染料标记肽和聚乙二醇的自组装异质单层进行功能化，已被开发用于在体内可视化蛋白水解活性。本文提出了一种一步合成策略，可简单地生成具有表面定义的 AuNP 探针库，以此作为调整和评估探针特性的手段，以实现蛋白酶激活后的最大荧光增强。针对胰蛋白酶和尿激酶型纤溶酶原激活剂的最佳 AuNP 探针需要掺入暗猝灭剂，以实现 5 至 8 倍的信号放大。这些探针在体内具有延长的循环时间，并在小鼠肿瘤模型中具有高图像对比度。
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