Solid-phase synthesis of a peptide derivative of thymosin alpha1 and initial studies on its (99m)Tc-radiolabelling.
Chem Biol Drug Des
; 70(1): 40-6, 2007 Jul.
Article
em En
| MEDLINE
| ID: mdl-17630993
ABSTRACT
A derivative (1) of the immunopotentiating 28-peptide thymosin alpha1 has been especially designed, so that it can be (99m)Tc-radiolabelled, and synthesized following the Fmoc solid-phase peptide synthesis approach. Derivative 1 contains the N-terminal fragment Talpha1[1-14] as a bioactive segment, at the C-terminus of which a (99m)Tc-chelating moiety consisting of N(alpha),N(alpha)-dimethylglycine, serine and cysteine is linked through the N(epsilon)-amino group of a 'bifunctional' lysine residue; the latter is indirectly anchored on the solid-phase peptide synthesis resin through 6-aminocaproic acid (dmGSCK{N(epsilon)-Talpha1[1-14]}Aca). Synthetic derivative 1 was obtained at high overall yield (approximately 35%) and purity (>95%) and shown to be efficiently radiolabelled with (99m)Tc, thus resulting in the first, to our knowledge, so far reported (99m)Tc-radiolabelled derivative of thymosin alpha1, which may be eventually used as a specific molecular tool for the in vitro/in vivo study of the mode of action of the parent bioactive peptide.
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Base de dados:
MEDLINE
Assunto principal:
Peptídeos
/
Timosina
/
Compostos de Organotecnécio
/
Compostos Radiofarmacêuticos
Limite:
Animals
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article