1,720,986 research outputs found

    TWENTY YEARS OF NON-PEPTIDE CCK1 RECEPTOR ANTAGONISTS: ALL THAT GLITTERS IS NOT GOLD

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    During the last 20 years, pharmaceutical industry and academic eforts have led to several structurally unrelated classes of non peptide cholecystokinin-1 receptor antagonista. Due to the lack of high resolution structure of CCK1-R and its peptide ligand, different strategies to design antagonists have been adopted

    2D-QSAR and 3D-QSAR/CoMFA analyses of the N-terminal substituted anthranilic acid based CCK1 receptor antagonists: ‘Hic Rhodus, hic saltus’

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    A research is presented on quantitative structure–activity relationship (QSAR) studies on the more recent class of non-peptidic CCK1 receptor antagonists. Our results suggest that the balance of hydrophobicity and volume dependent polarizability term plays a key role in the antagonism of CCK1 receptor

    ANTHRANILIC ACID BASED CCK1 RECEPTOR ANTAGONISTS AND CCK-8 HAVE A COMMON STEP IN THEIR "RECEPTOR DESMODYNAMIC PROCESSES"

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    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
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