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  • Title: Anthranilic acid based CCK1 receptor antagonists and CCK-8 have a common step in their "receptor desmodynamic processes".
    Author: De Luca S, Saviano M, Lassiani L, Yannakopoulou K, Stefanidou P, Aloj L, Morelli G, Varnavas A.
    Journal: J Med Chem; 2006 Apr 20; 49(8):2456-62. PubMed ID: 16610788.
    Abstract:
    The interaction between the 1-47 N-terminus of the CCK(1)-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 CCK(1)-R like that of the endogenous ligand CCK-8. This specific interaction was not found in other nonpeptide ligands of the CCK(1)-R. Conformational studies, using NMR and energy minimization procedures, have allowed formulation of a new hypothesis on the CCK(1)-R binding mode of the anthranilic antagonists.
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