PEGylation and biodistribution of an anti-MUC1 aptamer in MCF-7 tumor-bearing mice.
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.
Department of Chemistry and Analytical Sciences, The Open University, MK7 6AA Milton Keynes, UK. c.dapieve@open.ac.uk
Chiara
C
Da Pieve
Elaine
E
Blackshaw
Sotiris
S
Missailidis
Alan C
AC
Perkins
D000818:Animals; D052157:Aptamers, Nucleotide / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics*; D006801:Humans; D061986:MCF-7 Cells; D051379:Mice; D015394:Molecular Structure; D018396:Mucin-1; D009368:Neoplasm Transplantation; D009374:Neoplasms, Experimental / Q000378:metabolism*; D011092:Polyethylene Glycols / Q000737:chemistry / Q000378:metabolism* / Q000493:pharmacokinetics; D017556:Technetium Compounds / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics; D014018:Tissue Distribution; D014183:Transplantation, Heterologous
D052157:Aptamers, Nucleotide; D018396:Mucin-1; D017556:Technetium Compounds; D011092:Polyethylene Glycols