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Design and synthesis of specific colevelin derivatives for in vitro and in vivo studies
Kostomoiri, M. ; Zikos, C. ; Benaki, D. ; Slaninová, Jiřina ; Pirmettis, I. ; Papadopoulos, M. ; Pelecanou, M. ; Livaniou, E.
Colivelin is the most potent member of the humanin family of neuroprotective peptides with in vitro and in vivo action against insults associated with Alzeimer’s Disease. The mechanism of action of colivelin is not yet elucidated. The objective of the present study is the design and synthesis of specific colivelin derivatives that can be used as molecular probes in in vitro and in vivo biological experiments. In the frame of the study three colivelin derivatives bearing suitable tags, i.e the fluorescent moiety FITC, the 99mTc-radiometal chelating unit dimethylGly-Ser-Cys, and the streptavidin-counterpart biotinyl-group, were designed and synthesized. These derivatives will be used in in vitro cell component binding and in vivo biodistribution experiments, in order to gain better insight on the mode of the neuroprotective action of colivelin.
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In vitro and in vivo studies of the neuroprotective peptide humanin using 125I-radiolabeled humanin derivatives
Evangelou, A. ; Zikos, C. ; Benaki, D. ; Pelecanou, M. ; Bouziotis, P. ; Papadopoulos, M. ; Borovičková, Lenka ; Veselá, Iva ; Elbert, Tomáš ; Kunešová, G. ; Pirmettis, I. ; Paravatou-Petsotas, M. ; Slaninová, Jiřina ; Livaniou, E.
Four new HN-derivatives were synthesized: Y-PAGASRLLLTGEIDLP (Y-des-Leu-RG-PAGA, 1), Y-PAGASRLLLLTGEIDLP (Y-RG-PAGA, 2), Y-SALLRSIPAPAGASRLLLTGEIDLP (Y-des-Leu-Colivelin, 3), Y-SALLRSIPAPAGASRLLLLTGEIDLP (Y-Colivelin, 4), their neuroprotective action was evaluated in the T-maze test and the most active ones were monoradioiodinated with 125I and the labelled peptides used for binding and biodistribution studies.
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