PEGylation and Biodistribution of an anti-MUC1 Aptamer in MCF-7 Tumor-Bearing Mice

被引：64

作者：

Da Pieve, Chiara ^{[1
]}

Blackshaw, Elaine ^{[2
]}

Missailidis, Sotiris ^{[1
]}

Perkins, Alan C. ^{[2
]}

机构：

[1] Open Univ, Dept Chem & Analyt Sci, Milton Keynes MK7 6AA, Bucks, England

[2] Univ Nottingham, Sch Clin Sci, Acad Med Phys, Nottingham NG7 2UH, England

来源：

BIOCONJUGATE CHEMISTRY | 2012年 / 23卷 / 07期

关键词：

DNA APTAMERS; DESIGN; CONJUGATION; TC-99M; MARKER;

D O I：

10.1021/bc300128r

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Aptamers are characterized by a rapid renal clearance leading to a short in vivo circulating half-life. In order to use aptamers as anticancer therapeutic agents, their exposure time to the tumor has to be enhanced via increasing residency in the bloodstream. A way to achieve this goal is by conjugating the aptamer to poly(ethylene glycol) (PEG). Herein, we present the conjugation of a bifunctionalized anti-MUC1 aptamer (NH2-AptA-SR) with the Tc-99m coordinating moiety MAG2 and either a conventional branched PEG or the comb-shaped PolyPEG via a two-step synthesis. The isolated products were radiolabeled with Tc-99m and their biodistribution and tumor-targeting properties in MCF-7 tumor bearing mice were analyzed and compared.

引用

页码：1377 / 1381

页数：5

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