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

• Main Authors: Chutima Jiarpinitnun, Laura L. Kiessling
• Other Authors: University of Wisconsin Madison
• Format: Article
• Published: 2018
• Subjects: Biochemistry, Genetics and Molecular Biology; Chemical Engineering; Chemistry; Medicine
• Online Access: https://repository.li.mahidol.ac.th/handle/123456789/28671
• Institution: Mahidol University

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. © 2010 American Chemical Society.