AI Article Synopsis
- Aptamers have a short circulation time in the body due to rapid kidney clearance, which limits their effectiveness as cancer therapies.
- To improve their effectiveness against tumors, researchers are exploring ways to extend their time in the bloodstream by attaching them to poly(ethylene glycol) (PEG).
- This study details the synthesis of a specific anti-MUC1 aptamer conjugated with a radiolabeling component and different types of PEG, followed by testing the resulting compounds in mice with breast tumors to evaluate their targeting ability and distribution.
Article Abstract
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 (NH(2)-AptA-SR) with the (99m)Tc 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 (99m)Tc and their biodistribution and tumor-targeting properties in MCF-7 tumor bearing mice were analyzed and compared.
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| http://dx.doi.org/10.1021/bc300128r | DOI Listing |
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