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Synthesis by High-Efficiency Liquid-Phase (HELP) Method of Oligonucleotides Conjugated with High-Molecular Weight
G M Bonora1, S Zaramella, F M Veronese
1University of Cagliari, Pharmaco-Chemico-Technological Department. Via Ospedale 72 - 09127 Cagliari. New Address (from 1999): University of Trieste, Dept. of Chemical Sciences-Via Giorgieri 1-34127-Trieste. Italy.University of Padova. Italy. bonora@chor.unipd.it
Abstract:
The chemical modification of synthetic oligonucleotides has recently been investigated to improve their pharmacological utilization. In addition to chemical alterations of the backbone and of the heterocyclic bases, their conjugation with amphiphylic moieties, such as the polyethylene glycol has been proposed. The large scale production of these molecules as demanded for commercial purposes is hampered by the heterogeneity of the solid-phase processes and by the low reactivity of high-molecular weight PEGs in solution. A new synthetic procedure based on the recently developed liquid-phase method (HELP), has been set up to overcome these limitations.
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