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

Research output: Contribution to journalArticle

12 Citations (Scopus)

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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Cholecystokinin Receptors
Sincalide
Ligands
Fluorescence Spectrometry
Fluorescence spectroscopy
Nuclear magnetic resonance
anthranilic acid

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Anthranilic acid based CCK1 receptor antagonists and CCK-8 have a common step in their "receptor desmodynamic processes". / De Luca, Stefania; Saviano, Michele; Lassiani, Lucia; Yannakopoulou, Konstantina; Stefanidou, Penny; Aloj, Luigi; Morelli, Giancarlo; Varnavas, Antonio.

In: Journal of Medicinal Chemistry, Vol. 49, No. 8, 20.04.2006, p. 2456-2462.

Research output: Contribution to journalArticle

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, vol. 49, no. 8, pp. 2456-2462. https://doi.org/10.1021/jm051050n
De Luca, Stefania ; Saviano, Michele ; Lassiani, Lucia ; Yannakopoulou, Konstantina ; Stefanidou, Penny ; Aloj, Luigi ; Morelli, Giancarlo ; Varnavas, Antonio. / Anthranilic acid based CCK1 receptor antagonists and CCK-8 have a common step in their "receptor desmodynamic processes". In: Journal of Medicinal Chemistry. 2006 ; Vol. 49, No. 8. pp. 2456-2462.
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