Role of sulfate ester in influencing biological activity of cholecystokinin-related peptides
In dispersed acini from guinea pig, mouse, or rat pancreas cholecystokinin-(27-33) is a full agonist, and removing the sulfate ester from the tyrosine residue in position 27 caused a 100- to 300-fold decrease in potency with no change in efficacy. In dispersed acini from mouse or rat pancreas, cholecystokinin-(27-32)-NH2 is a partial agonist, and removing the sulfate ester from the tyrosine in position 27 abolished the efficacy. The desulfated peptide was able, however, to interact with ( SVI) CCK receptors with a potency that was threefold less than that of cholecystokinin-(27-32)-NH2 and therefore functioned as a cholecystokinin receptor antagonist. In dispersed acini from guinea pig pancreas cholecystokinin-(27-32)-NH2 is a cholecystokinin receptor antagonist. Removing the sulfate ester from the tyrosine residue in position 27 of cholecystokinin-(27-32)-NH2 caused a fourfold decrease in potency but did not abolish the ability of the peptide to interact with cholecystokinin receptors; therefore, desulfated cholecystokinin-(27-32)-NH2 functioned as a cholecystokinin receptor antagonist.
- Research Organization:
- National Institutes of Health, Bethesda, MD
- OSTI ID:
- 6294725
- Journal Information:
- Am. J. Physiol.; (United States), Journal Name: Am. J. Physiol.; (United States) Vol. 252:2; ISSN AJPHA
- Country of Publication:
- United States
- Language:
- English
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62 RADIOLOGY AND NUCLEAR MEDICINE
AMYLASE
ANIMALS
BETA DECAY RADIOISOTOPES
BIOCHEMISTRY
BODY
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DAYS LIVING RADIOISOTOPES
DIGESTIVE SYSTEM
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ELECTRON CAPTURE RADIOISOTOPES
ENDOCRINE GLANDS
ENZYMES
ESTERS
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GLYCOSYL HYDROLASES
GUINEA PIGS
HYDROLASES
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
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KININS
MAMMALS
MICE
NUCLEI
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ODD-EVEN NUCLEI
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OXYGEN COMPOUNDS
PANCREAS
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