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99mTc-labeling and in vitro characterization of N4- and N3S-RGDS-derivative peptides |
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| Authors: | A Perera Pintado S J Mather M A Stalteri D Allison A Prats Capote A Hernández Cairo O Reyes Acosta M Bequet Romero |
| Institution: | (1) Centre for Clinical Research, 34 No. 4501 and/ 45 and 47, Kohly, Playa, C. Habana, CP 11300, Cuba;(2) Department Nuclear Medicine, St Bartholomew’s Hospital, London, EC1A 7BE, UK;(3) Centre of Genetic Engineering and Biotechnology, 31 and/ 158 and 190, Cubanacan, Playa, C. Habana, CP 10600, Cuba |
| Abstract: | 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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