Importance of sulfation of gastrin or cholecystokinin (CCK) on affinity for gastrin and CCK receptors

Journal Article · Sat Jul 01 04:00:00 EDT 1989 · Peptides (Fayetteville, New York); (USA)

DOI:https://doi.org/10.1016/0196-9781(89)90114-9· OSTI ID:5085560

Huang, S C; Yu, D H; Wank, S A; Mantey, S; Gardner, J D; Jensen, R T ^[1]

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1. National Institute of Diabetes and Digestive and Kidney Diseases, Bethesda, MD (USA)

We investigated the importance of sulfation of gastrin or cholecystokinin (CCK) on influencing their affinity for gastrin or CCK receptors by comparing the abilities of sulfated gastrin-17 (gastrin-17-II), desulfated gastrin-17 (gastrin-17-I), CCK-8 and desulfated CCK-8 (des(SO3)CCK-8) to interact with CCK or gastrin receptors on guinea pig pancreatic acini. For inhibiting binding of 125I-gastrin to gastrin receptors, gastrin-17-II (Kd 0.08 nM) greater than CCK-8 (Kd 0.4 nM) greater than gastrin-17-I (Kd 1.5 nM) greater than des(SO3)CCK-8 (Kd 28 nM). For inhibiting binding of 125I-Bolton Hunter-labeled CCK-8 to CCK receptors the relative potencies were: CCK-8 much greater than des(SO3)CCK-8 = gastrin-17-II greater than gastrin-17-I. Each peptide interacted with both high and low affinity CCK binding sites. The relative abilities of each peptide to interact with high affinity CCK receptors showed a close correlation with their abilities to cause half-maximal stimulation of enzyme secretion. These results demonstrate that, in contrast to older studies, sulfation of both CCK and gastrin increase their affinities for both gastrin and CCK receptors. Moreover, the gastrin receptor is relatively insensitive to the position of the sulfate moiety, whereas the CCK receptor is extremely sensitive to both the presence and exact position of the sulfate moiety.

• OSTI ID: 5085560
• Journal Information: Peptides (Fayetteville, New York); (USA), Journal Name: Peptides (Fayetteville, New York); (USA) Vol. 10:4; ISSN PPTDD; ISSN 0196-9781
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
AMYLASE
ANIMALS
BETA DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BODY
DAYS LIVING RADIOISOTOPES
DIGESTIVE SYSTEM
ELECTRON CAPTURE RADIOISOTOPES
ENDOCRINE GLANDS
ENZYMES
GASTRIN
GLANDS
GLYCOSYL HYDROLASES
GUINEA PIGS
HORMONES
HYDROLASES
IN VITRO
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
KININS
MAMMALS
MEMBRANE PROTEINS
NUCLEI
O-GLYCOSYL HYDROLASES
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
OXYGEN COMPOUNDS
PANCREAS
PEPTIDE HORMONES
PEPTIDES
POLYPEPTIDES
PROTEINS
RADIOISOTOPES
REACTION KINETICS
RECEPTORS
RODENTS
SULFATES
SULFUR COMPOUNDS
TRACER TECHNIQUES
VERTEBRATES