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Protein & Peptide Letters

Editor-in-Chief

ISSN (Print): 0929-8665
ISSN (Online): 1875-5305

The Use of Tripeptides for Lead Discovery of 5-HT4 Receptor Ligands

Author(s): A. Hanna-Elias, P. E. Thompson, D. T. Manallack, H. R. Irving, I. M. Coupar, I. Berque-Bestel and M. N. Iskander

Volume 16, Issue 7, 2009

Page: [805 - 809] Pages: 5

DOI: 10.2174/092986609788681805

Price: $65

Abstract

A series of 30 tripeptides were synthesized and tested as novel 5-HT4 receptor ligands. Receptor binding assays showed that a subset of compounds had reasonable potency relative to the agonists serotonin and 5-methoxytryptamine. Structure-activity analyses and molecular docking have highlighted avenues for further synthetic work.

Keywords: Serotonin, 5-HT, 5-HT4, tripeptide, molecular docking, radioligand binding


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