Anthranilic acid based CCK1 receptor antagonists and CCK-8 have a common step in their "receptor desmodynamic processes"

Stefania De Luca, Michele Saviano, Lucia Lassiani, Konstantina Yannakopoulou, Penny Stefanidou, Luigi Aloj, Giancarlo Morelli, Antonio Varnavas

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Abstract

The interaction between the 1-47 N-terminus of the CCK1-R and the anthranilic acid based antagonists has been investigated by fluorescence spectroscopy. These antagonists interact with W39 of the N-terminal domain of the CCK1-R like that of the endogenous ligand CCK-8. This specific interaction was not found in other nonpeptide ligands of the CCK1-R. Conformational studies, using NMR and energy minimization procedures, have allowed formulation of a new hypothesis on the CCK1-R binding mode of the anthranilic antagonists.

Original languageEnglish
Pages (from-to)2456-2462
Number of pages7
JournalJournal of Medicinal Chemistry
Volume49
Issue number8
DOIs
Publication statusPublished - Apr 20 2006

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ASJC Scopus subject areas

  • Organic Chemistry

Cite this

De Luca, S., Saviano, M., Lassiani, L., Yannakopoulou, K., Stefanidou, P., Aloj, L., Morelli, G., & Varnavas, A. (2006). Anthranilic acid based CCK1 receptor antagonists and CCK-8 have a common step in their "receptor desmodynamic processes". Journal of Medicinal Chemistry, 49(8), 2456-2462. https://doi.org/10.1021/jm051050n