A “Ready-To-Use” fluorescent-labelled-cysteine-TBTP (4-thiobutyltriphenylphosphonium) synthon to investigate the delivery of non-permeable PNA (Peptide Nucleic …

…, S Caldarelli, A Di Giorgio, T Barouillet, A Doglio…

Index: Mehiri, Mohamed; Caldarelli, Sergio; Giorgio, Audrey Di; Barouillet, Thibault; Doglio, Alain; Condom, Roger; Patino, Nadia Bioorganic Chemistry, 2007 , vol. 35, # 4 p. 313 - 326

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Citation Number: 6

Abstract

This paper reports:(i) the facile synthesis of a cysteine synthon incorporating both a fluorescent group and a triphenylphosphonium derivative (TBTP) via the formation of a disulphide bond, which can subsequently undergo facile intracellular scission,(ii) the direct conjugation of this synthon to a non-permeable drug,(a cyclic PNA (peptide nucleic acid)- based compound has been chosen as a model), and (iii) that this conjugation enables the ...