99mTc-labeling and in vitro characterization of N4- and N3S-RGDS-derivative peptides

被引：0
|
作者：
A. Perera Pintado
S. J. Mather
M. A. Stalteri
D. Allison
A. Prats Capote
A. Hernández Cairo
O. Reyes Acosta
M. Bequet Romero
机构：
[1] Centre for Clinical Research,Department Nuclear Medicine
[2] St Bartholomew’s Hospital,undefined
[3] Centre of Genetic Engineering and Biotechnology,undefined
来源：
Journal of Radioanalytical and Nuclear Chemistry | 2008年 / 275卷
关键词：
Peptide; High Performance Liquid Chromatography; Hybrid Peptide; Trifluoracetic Acid; Stannous Fluoride;
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摘要：
The aim of this work was to characterize the in vitro behavior of N4- and N3S-RGDS-derivative peptides labeled with 99mTc. Peptides AGGG-Abu-GRGDSPK-NH2 (F22) and C(acm)-GGG-Abu-GRGDSPK-NH2 (SMA1) were synthesized by solid phase. The stability of 99mTc-labeled peptides was assessed in a 30-fold molar excess of cysteine and in plasma. The affinity for plasma proteins was also evaluated. Labeling yield was >95% for both peptides. 99mTc-F22 was not stable in presence of cysteine, but 63% of 99mTc remained chelated to SMA1 up to 24 hours. Both peptides showed low affinity to plasma proteins. N3S-RGDS-derivative peptide (SMA1) showed more stable coordination binding with 99mTc and a higher stability in plasma with regard to N4-RGDS-derivative peptide (F22).
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页码：619 / 626
页数：7
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