Abstract
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 188Re, furthermore the in vitro/in vivo stability was evaluated accordingly. The labelling yield of the conjugate G5-FA-DTPA-188Re 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.
Keywords: Dendrimer, Folic acid, PAMAM, Radiolabelled, Rhenium, polyamido amine, Rhenium-188, micro-SPECT, in vitro, fluorescein
Medicinal Chemistry
Title:Synthesis and 188Re Radiolabelling of Dendrimer Polyamide Amine (PAMAM) Folic Acid Conjugate
Volume: 8 Issue: 4
Author(s): Wei Cui, Yuanqing Zhang, Xiaoping Xu and Yu-Mei Shen
Affiliation:
Keywords: Dendrimer, Folic acid, PAMAM, Radiolabelled, Rhenium, polyamido amine, Rhenium-188, micro-SPECT, in vitro, fluorescein
Abstract: 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 188Re, furthermore the in vitro/in vivo stability was evaluated accordingly. The labelling yield of the conjugate G5-FA-DTPA-188Re 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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Cite this article as:
Cui Wei, Zhang Yuanqing, Xu Xiaoping and Shen Yu-Mei, Synthesis and 188Re Radiolabelling of Dendrimer Polyamide Amine (PAMAM) Folic Acid Conjugate, Medicinal Chemistry 2012; 8 (4) . https://dx.doi.org/10.2174/157340612801216256
DOI https://dx.doi.org/10.2174/157340612801216256 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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