In:
Journal of Peptide Science, Wiley, Vol. 14, No. 12 ( 2008-12), p. 1251-1258
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‐NH 2 and Ac‐HMWLYF‐NH 2 —that exhibited agonistic activity. Although the corresponding affinities were relatively low (EC 50 values of 146 and 6.7 µ M , 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 [ 35 S]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.
Type of Medium:
Online Resource
ISSN:
1075-2617
,
1099-1387
Language:
English
Publisher:
Wiley
Publication Date:
2008
detail.hit.zdb_id:
1491819-5
SSG:
12
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