Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P01350 (gastrin)
 9,683 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Guanylate cyclase in the guinea pig fundic mucosa occurred in two enzymatic forms: a "soluble" form and a particulate form. The mean basal activity of the soluble fraction measured in the presence of 300 micrometer guanosine-5'-triphosphate and 5 mM MnCl2 was 72.6 +/- 5.3 pmoles of cyclic GMP per mg of protein per min. Guanylate cyclase activity was dependent on Mn2+; it was increased by sodium azide (NaN3), CaCl2, cysteine, secretin, and cholecystokinin, but it was not influenced by gastrin, histamine, cholinergic esters, prostaglandins E1 and A1. NaN3 (1 mM) decreased the apparent Km for MnCl2 and potentiated the effects of MgCl2. The activity of the particulate fraction represented about 14% of that of the supernatant fraction. The guanylate cyclase activity of that fraction was not modified by NaN3, gastrin, cholinergic agents, secretin, or cholecystokinin. Cysteine inhibited its activity. These data do not support the hypothesis that cyclic GMP acts as a second messenger for the action of cholinergic agents and gastrin in the guinea pig gastric mucosa.
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PMID:Effect of Ca2+, Mg2+, NaN3, cholinergic agents, and gastrointestinal hormones on the guanylate cyclase from guinea pig gastric mucosa. 2 35

The interrelationship of the effects of antacids and of rising intragastric pH on serum gastrin levels was examined by comparing the effect of three antacids (Mg(OH)2Al(OH)3, and CaCO3), and their nonbuffering chloride compounds (MgCl2, AlCl3, and CaCl2), on serum gastrin and intragastric pH in duodenal ulcer patients. In the case of calcium, the effect of CaCl2 with a pH of 10, and in another group, CaCl2 with a pH of 2, was studied. In the case of magnesium, a control group was also investigated. In another group, the effect of a nonionized suspension (BaSO4) was studied in order to assess the contribution of intragastric volume. Serum gastrin was determined radioimmunologically, and pH measurements were performed in vitro using a glass electrode. Serum gastrin concentrations rose significantly whenever intragastric pH was raised. Serum gastrin also rose after MgCl2, AlCl3, and CaCl2 with a pH of 2, when intragastric pH was not significantly altered. This rise, however, was significantly smaller than after administration of the antacids, except in the MgCl2-Mg(OH)2 and in the CaCl2 pH 10-CaCO3 groups. No significant rise of serum gastrin levels was observed after BaSO4. In nonulcer subjects, gastrin response was smaller than in the duodenal ulcer patients. The results suggest that administration of nonbuffering Mg-, Al-, and Ca-chlorides leads to elevated serum gastrin levels in duodenal ulcer patients; rising intragastric pH, however, exerts an additional serum gastrin response.
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PMID:Effect of rising intragastric pH induced by several antacids on serum gastrin concentrations in duodenal ulcer patients and in a control group. 23

The experiments have been carried out on four intact awake dogs to study the influence of intragastric introduction of deionized water, 5 mmol/l of calcium and magnesium chloride solutions in a dose of 3 ml/kg on release of gastrin and insulin into blood. It is stated that during the first 4 min after infusion of deionized water the release of gastrin decreases by 89 +/- 32 conventional units (c.u.), CaCl2 exerts a more pronounced inhibitory effect (168 +/- 36 c.u.), while MgCl2, on the contrary, increases the gastrin release by 398 +/- 92 c.u. Atropin (0.03 mg/kg, subcutaneous injection, 10 min before infusion) absolutely takes away the gastrin-stimulating effect of magnesium, but it has almost no influence on the gastrin-inhibitory effect of calcium. The latter can be taken away by 62% by ornid (5 mg/kg subcutaneously, 20 min before infusion). Preliminary anaesthesia of the stomach mucosa by trymecain or novocain absolutely remove the effect of both calcium and magnesium. Insulin release remained significantly unchanged in any series of experiments.
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PMID:[An analysis of the mechanism of the effect of intragastric calcium and magnesium on the release of gastrin and insulin in dogs]. 128 91

[3H]L-365,260, [(3R-(+)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4- benzodiazepin-3-yl)-N'-(3-methylphenyl)urea], a new potent and selective nonpeptide brain cholecystokinin (CCK-B) and gastrin receptor antagonist, bound saturably and reversibly to guinea pig brain membranes. Scatchard analysis indicated a single class of high affinity (Kd = 2.3 nM) binding sites. The binding of [3H]L-365,260 was stereospecific, because unlabeled L-365,260 (an R-enantiomer) was approximately 100 times more potent than its S-enantiomer in displacing binding. The relative potencies of various CCK/gastrin-related peptides and nonpeptide peripheral CCK-A antagonists in displacing [3H]L-365,260 brain binding correlated with their potencies in displacing the binding of 125I-CCK to brain receptors but not their potencies in displacing the peripherally selective CCK-A ligand [3H]L-364,718 from pancreatic receptors. The regional distribution of [3H]L-365,260 binding in various brain areas correlated with 125I-CCK binding. Specific [3H]L-365,260 binding to guinea pig brain membranes was reduced by omission of NaCl but was not affected by omission of MgCl2 or addition of guanosine 5'-(beta-gamma-imido)triphosphate or various pharmacological agents known to interact with other common peptide and nonpeptide receptor systems. [3H]L-365,260 also bound in a specific manner to guinea pig gastric glands but only negligibly to guinea pig or rat pancreas. The binding of [3H]L-365,260 to gastric glands was inhibited by CCK/gastrin antagonists with potencies similar to those for inhibition of 125I-gastrin binding in this tissue. Collectively, the data indicates that [3H]L-365,260 represents a new potent nonpeptide antagonist radioligand suitable for the study of brain CCK-B and gastrin receptors.
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PMID:Characterization of the binding of [3H]L-365,260: a new potent and selective brain cholecystokinin (CCK-B) and gastrin receptor antagonist radioligand. 273 96

Gastrin was recently shown to be phosphorylated on its single tyrosine by the epidermal growth factor (EGF)-stimulated tyrosine protein kinase (TPK). The TPK previously detected in the murine lymphoma (LSTRA) induced by the Moloney murine leukemia virus phosphorylates gastrin, the apparent Km is 65 microM and the maximum rate 1900 pmol/min per mg; the kinase is more efficient with MnCl2 than with MgCl2, is stimulated by NaVO3 and inhibited by ZnCl2. Gastrin phosphorylation is observed only when a TPK is expressed by the cell: extracts of fibroblasts infected with a temperature-sensitive mutant of the Rous sarcoma virus had no gastrin kinase activity when grown at the non-permissive temperature whereas cells grown at the permissive temperature were transformed and disclosed a clear gastrin kinase activity. Gastrin kinases were detected in various transformed cells: human lymphomas, K562 cells, cells from a patient with acute proliferative leukemia, and normal cells: human T and B lymphocytes.
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PMID:Detection of tyrosine-specific protein kinases with gastrin as exogenous substrate. 384 96