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- W2078009178 abstract "A combinatorial peptide library contains an enormous combination of amino acid sequences and drug candidates, but an effective screening strategy to identify a variety of bioactive peptides has yet to be established. In this article, a random hexapeptide library was screened to identify novel peptide ligands for a 5-oxo-ETE receptor (OXER), which is a G-protein-coupled receptor for bioactive lipids, by using an OXER-Gi1α fusion protein. We successfully identified 2 hexapeptides—Ac-HMQLYF-NH2 and Ac-HMWLYF-NH2—that exhibited agonistic activity. Although the corresponding affinities were relatively low (EC50 values of 146 and 6.7 µM, respectively), the activities were confirmed by other independent cell-based assay methods, namely, intracellular calcium mobilization and cell chemotaxis. This study demonstrates that a combinatorial peptide library may be screened using a [35S]GTPγS binding assay with G-protein-coupled receptor (GPCR)–Gα fusion proteins, in general, and that of peptide ligands can be obtained even for nonpeptide receptors. Copyright © 2008 European Peptide Society and John Wiley & Sons, Ltd." @default.
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- W2078009178 date "2008-12-01" @default.
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- W2078009178 title "Identification of novel peptide agonists from a random peptide library for a 5-oxo-ETE receptor, a receptor for bioactive lipids" @default.
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- W2078009178 doi "https://doi.org/10.1002/psc.1064" @default.
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