Document Detail


Anthranilic acid based CCK1 receptor antagonists and CCK-8 have a common step in their "receptor desmodynamic processes".
MedLine Citation:
PMID:  16610788     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Stefania De Luca; Michele Saviano; Lucia Lassiani; Konstantina Yannakopoulou; Penny Stefanidou; Luigi Aloj; Giancarlo Morelli; Antonio Varnavas
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  49     ISSN:  0022-2623     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2006 Apr 
Date Detail:
Created Date:  2006-04-13     Completed Date:  2006-05-22     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2456-62     Citation Subset:  IM    
Affiliation:
Interuniversity Research Center on Bioactive Peptides (CIRPeB), University of Naples Federico II, and Institute of Biostructures and Bioimaging of CNR, Via Mezzocannone, 16 I-80134 Naples, Italy.
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MeSH Terms
Descriptor/Qualifier:
Animals
Anthranilic Acids / chemistry*,  pharmacology*
Binding, Competitive / drug effects
Biological Assay
Humans
Indoles / chemistry,  pharmacology
Ligands
Magnetic Resonance Spectroscopy
Models, Molecular
Molecular Structure
Pancreas / drug effects,  metabolism
Proglumide / analogs & derivatives,  chemistry,  pharmacology
Protein Conformation
Rats
Receptor, Cholecystokinin A / antagonists & inhibitors*,  chemistry
Sincalide / chemistry,  pharmacology*
Spectrometry, Fluorescence
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Anthranilic Acids; 0/Indoles; 0/Ligands; 0/Receptor, Cholecystokinin A; 0/VL-0395; 107097-80-3/loxiglumide; 118-92-3/anthranilic acid; 25126-32-3/Sincalide; 6620-60-6/Proglumide

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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