PEGylation and biodistribution of an anti-MUC1 aptamer in MCF-7 tumor-bearing mice |
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Authors: | Da Pieve Chiara Blackshaw Elaine Missailidis Sotiris Perkins Alan C |
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Institution: | Department of Chemistry and Analytical Sciences, The Open University, MK7 6AA Milton Keynes, UK. c.dapieve@open.ac.uk |
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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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