Solid-Phase Synthesis of PEGylated Lipopeptides Using Click Chemistry

Rasmus Irming Jølck; Rolf Henrik Berg; Thomas Lars Andresen

doi:10.1021/bc100002a

Solid-Phase Synthesis of PEGylated Lipopeptides Using Click Chemistry

Rasmus Irming Jølck, Rolf Henrik Berg, Thomas Lars Andresen

Research output: Contribution to journal › Journal article › Research › peer-review

Abstract

A versatile methodology for efficient synthesis of PEGylated lipopeptides via CuAAC “Click” conjugation between alkyne-bearing solid-supported lipopeptides and azido-functionalized PEGs is described. This new and very robust method offers a unique platform for synthesizing PEGylated lipopeptides with a high level of complexity. These molecules, obtained in a single purification step, are ideally suited for functionalization of solid-supported lipid bilayers and liposomal drug delivery systems and are particularly valuable in enzyme activation strategies.

Original language	English
Journal	Bioconjugate Chemistry
Volume	21
Issue number	5
Pages (from-to)	807-810
ISSN	1043-1802
DOIs	https://doi.org/10.1021/bc100002a
Publication status	Published - 2010

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abstract = "A versatile methodology for efficient synthesis of PEGylated lipopeptides via CuAAC “Click” conjugation between alkyne-bearing solid-supported lipopeptides and azido-functionalized PEGs is described. This new and very robust method offers a unique platform for synthesizing PEGylated lipopeptides with a high level of complexity. These molecules, obtained in a single purification step, are ideally suited for functionalization of solid-supported lipid bilayers and liposomal drug delivery systems and are particularly valuable in enzyme activation strategies.",

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AU - Jølck, Rasmus Irming

AU - Berg, Rolf Henrik

AU - Andresen, Thomas Lars

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N2 - A versatile methodology for efficient synthesis of PEGylated lipopeptides via CuAAC “Click” conjugation between alkyne-bearing solid-supported lipopeptides and azido-functionalized PEGs is described. This new and very robust method offers a unique platform for synthesizing PEGylated lipopeptides with a high level of complexity. These molecules, obtained in a single purification step, are ideally suited for functionalization of solid-supported lipid bilayers and liposomal drug delivery systems and are particularly valuable in enzyme activation strategies.

AB - A versatile methodology for efficient synthesis of PEGylated lipopeptides via CuAAC “Click” conjugation between alkyne-bearing solid-supported lipopeptides and azido-functionalized PEGs is described. This new and very robust method offers a unique platform for synthesizing PEGylated lipopeptides with a high level of complexity. These molecules, obtained in a single purification step, are ideally suited for functionalization of solid-supported lipid bilayers and liposomal drug delivery systems and are particularly valuable in enzyme activation strategies.

U2 - 10.1021/bc100002a

DO - 10.1021/bc100002a

M3 - Journal article

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JO - Bioconjugate Chemistry

JF - Bioconjugate Chemistry

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Solid-Phase Synthesis of PEGylated Lipopeptides Using Click Chemistry

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