Unexpected Enhancement in Biological Activity of a GPCR Ligand Induced by an Oligoethylene Glycol Substituent

作者:Jiarpinitnun Chutima; Kiessling Laura L*
来源:Journal of the American Chemical Society, 2010, 132(26): 8844-+.
DOI:10.1021/ja102640c

摘要

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.

  • 出版日期2010-7-7