Solid-phase synthesis of a peptide derivative of thymosin alpha1 and initial studies on its (99m)Tc-radiolabelling |
| |
Authors: | Klimentzou Persefoni Beck Alexander Varvarigou Alexandra Tsitsilonis Ourania Voelter Wolfgang Pirmettis Ioannis Papadopoulos Minas Livaniou Evangelia Zikos Christos |
| |
Affiliation: | National Centre for Scientific Research 'Demokritos', Aghia Paraskevi Attikis, Athens 15310, Greece. |
| |
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. |
| |
Keywords: | 99mTc‐chelating moiety 99mTc‐radiolabelling Fmoc solid‐phase peptide synthesis thymosin alpha1 |
本文献已被 PubMed 等数据库收录! |
|