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Unexpected enhancement in biological activity of a GPCR ligand induced by an oligoethylene glycol substituent.

ABSTRACT: Polyethylene glycol (PEG) is widely used, and many biologically active molecules are modified with oligoethylene glycol substituents to enhance their half-lives in circulation. The pervasive use of PEG substituents is partly due to their presumed inertness. Our investigation of formyl peptide receptor (FPR)-mediated chemotaxis reveals that oligoethylene glycol substitution can enhance the ability of the peptide chemoattractant N-formyl-methionine-leucine-phenylalanine (fMLF) to activate signal transduction through FPR, a transmembrane G-protein-coupled receptor.

SUBMITTER: Jiarpinitnun C

PROVIDER: S-EPMC2913153 | biostudies-literature | 2010 Jul

REPOSITORIES: biostudies-literature

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Unexpected enhancement in biological activity of a GPCR ligand induced by an oligoethylene glycol substituent.

Jiarpinitnun Chutima C Kiessling Laura L LL

Journal of the American Chemical Society 20100701 26

Polyethylene glycol (PEG) is widely used, and many biologically active molecules are modified with oligoethylene glycol substituents to enhance their half-lives in circulation. The pervasive use of PEG substituents is partly due to their presumed inertness. Our investigation of formyl peptide receptor (FPR)-mediated chemotaxis reveals that oligoethylene glycol substitution can enhance the ability of the peptide chemoattractant N-formyl-methionine-leucine-phenylalanine (fMLF) to activate signal t ...[more]

PMID: 20536128

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