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

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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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Authors and Affiliations

  1. Centre for Clinical Research, 34 No. 4501 and/ 45 and 47, Kohly, Playa, C. Habana, CP 11300, Cuba

    A. Perera Pintado, A. Prats Capote & A. Hernández Cairo

  2. Department Nuclear Medicine, St Bartholomew’s Hospital, London, EC1A 7BE, UK

    S. J. Mather, M. A. Stalteri & D. Allison

  3. Centre of Genetic Engineering and Biotechnology, 31 and/ 158 and 190, Cubanacan, Playa, C. Habana, CP 10600, Cuba

    O. Reyes Acosta & M. Bequet Romero

Authors
  1. A. Perera Pintado
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  2. S. J. Mather
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  3. M. A. Stalteri
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  4. D. Allison
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  5. A. Prats Capote
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  6. A. Hernández Cairo
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  7. O. Reyes Acosta
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  8. M. Bequet Romero
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Correspondence to A. Perera Pintado.

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Perera Pintado, A., Mather, S.J., Stalteri, M.A. et al. 99mTc-labeling and in vitro characterization of N4- and N3S-RGDS-derivative peptides. J Radioanal Nucl Chem 275, 619–626 (2008). https://doi.org/10.1007/s10967-007-6867-y

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  • DOI: https://doi.org/10.1007/s10967-007-6867-y

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