Journal
MEDICINAL CHEMISTRY
Volume 8, Issue 4, Pages 727-731Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/157340612801216256
Keywords
Dendrimer; Folic acid; PAMAM; Radiolabelled; Rhenium
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Funding
- Major Projects in National Science and Technology, Creation of major new drugs [2011ZX09501-001-05]
- National Nature Science Foundation of China [81071250]
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Folic acid receptors (FR) are usually over expressed in many cancer cells and are considered as potential targeted therapy agent. Generation of five polyamido amine (PAMAM) dendrimer folic acid conjugate was synthesised and radiolabelled with Re-188, furthermore the in vitro/in vivo stability was evaluated accordingly. The labelling yield of the conjugate G5-FA-DTPA-Re-188 was 67.1 % and its radiochemical purity exceeded 95 %. The conjugate also showed high in vitro stability and potential value for further structure modifications and evaluations.
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