PMID: 6172156Dec 18, 1981Paper

The importance of the amino acid in position 32 of cholecystokinin in determining its interaction with cholecystokinin receptors on pancreatic acini

Biochimica Et Biophysica Acta
G Z PanJ D Gardner

Abstract

In the C-terminal heptapeptide of cholecystokinin, replacement of the penultimate residue, aspartic acid, by beta-alanine caused a 300-fold decrease in the potency with which the peptide stimulated enzyme secretions, whereas replacement by glutamic acid caused a 1000-fold decrease in potency. The beta-alanine-substituted peptide was approximately ten times more potent when the n terminus was blocked with t-butyloxycarbonyl than when it was blocked with benzyloxycarbonyl, and the glutamic acid-substituted peptide was approximately twice as potent when the N terminus was blocked with t-butyloxycarbonyl than when it was blocked with benzyloxycarbonyl. Changes in the ability of the peptide to stimulate amylase secretion were accompanied by corresponding changes in the ability of the peptide to inhibit binding of 125I-labeled cholecystokinin. The magnitude of stimulation of enzyme secretion caused by a maximally effective peptide concentration was the same with each analogue as it was with the unaltered peptide. Replacing the aspartyl residue by beta-alanine or glutamic acid or replacing the N-terminal t-butyloxycarbonyl moiety by benzyloxycarbonyl caused an equivalent decrease in the ability of the peptide to stimulate enzyme secre...Continue Reading

References

Aug 1, 1975·The Journal of Clinical Investigation·J D GardnerM A Ondetti
May 14, 1968·Proceedings of the Royal Society of London. Series B, Containing Papers of a Biological Character·J S Morley
Apr 1, 1980·Proceedings of the National Academy of Sciences of the United States of America·R T JensenJ D Gardner

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Citations

Nov 10, 1992·European Journal of Pharmacology·L MaletínskáJ Martinez
Apr 12, 2003·Pharmacology & Toxicology·Eric S DawsonTerry P Lybrand
May 1, 1990·International Journal of Peptide and Protein Research·M RodriguezJ Martinez
Apr 1, 1986·International Journal of Peptide and Protein Research·J LaurJ Martinez
May 25, 1983·Biochimica Et Biophysica Acta·R T JensenJ D Gardner

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