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 , M. N. Iskander .

Journal Name: Protein & Peptide Letters

Volume 16 , Issue 7 , 2009

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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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Article Details

VOLUME: 16
ISSUE: 7
Year: 2009
Page: [805 - 809]
Pages: 5
DOI: 10.2174/092986609788681805
Price: $58

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