Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 3, Pages 927-931Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.12.075
Keywords
Dendrimer PAMAM; Radiolabeling; Folate receptor; Micro-SPECT imaging
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Funding
- Chinese Academy of Sciences [26200601]
- National Natural Science Foundation of China [10905087]
- Natural Science Foundation of Shanghai [3109ZR1438400]
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Acetylated (Ac) dendrimer poly(amido)-amine (PAMAM) generation 5 (G5) reacted with folic acid (FA), followed by reacting with 2-(p-isothiocyanatobenzyl)-6-methyl-diethylenetria minepentaacetic acid (1B4M DTPA) to form the conjugate of Ac-G5-FA-1B4M DTPA which was further radiolabeled with Tc-99m. The radiochemical yield is up to 98.9% with excellent in vitro/in vivo stability, rapid blood clearance and certain tumor accumulation which was further confirmed by micro-SPECT imaging study. (c) 2009 Elsevier Ltd. All rights reserved.
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