Page last updated: 2024-11-12

gastrin 17

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

gastrin-17 : One of the primary forms of gastrin that is a 17-membered peptide consisting of Glp, Gly, Pro, Trp, Leu, Glu, Glu, Glu, Glu, Glu, Ala, Tyr, Gly, Trp, Met, Asp and Phe-NH2 residues joined in sequence. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID16162108
CHEMBL ID4451154
CHEBI ID75441
MeSH IDM0061384

Synonyms (35)

Synonym
60748-06-3
heptadecapeptide gastrin
gastrin-17
little gastrin
gastrin i human, >=95% (hplc)
gastrin heptadecapeptide
g 17
gastrin 17
shg17ns
little gastrin i
18-34-gastrin, 18-(5-oxo-l-proline)-
10047-33-3
5-oxo-l-prolylglycyl-l-prolyl-l-tryptophyl-l-leucyl-l-alpha-glutamyl-l-alpha-glutamyl-l-alpha-glutamyl-l-alpha-glutamyl-l-alpha-glutamyl-l-alanyl-l-tyrosylglycyl-l-tryptophyl-l-methionyl-l-alpha-aspartyl-l-phenylalaninamide
glp-gly-pro-trp-leu-glu-glu-glu-glu-glu-ala-tyr-gly-trp-met-asp-phe-nh2
CHEBI:75441
c97h124n20o31s
gastrin i human
gastrin i (human) ,
gtpl8408
desulfated gastrin-17
AKOS024457376
CHEMBL4451154 ,
mfcd00076500
gastrin-i (human)
gastrin-1
gastrinihuman
Q6652696
A11815
AS-56740
gastrini,human
bdbm50517370
DTXSID601028770
(x = glp, phe-17 = c-terminal amide)
xgpwleeeeeaygwmdf
HB3575

Research Excerpts

Overview

Gastrin 17 is a growth factor for pancreatic, stomach and colorectal cancers. Gastrin 17 (G17) is a potent stimulant of gastric acid secretion in vivo.

ExcerptReferenceRelevance
"Gastrin 17 is a growth factor for pancreatic, stomach and colorectal cancers, and a potent stimulator of gastric acid secretion.The anti-gastrin immunogen, G17DT, consists of a large carrier protein, called Diptheria Toxoid (DT)."( Gastrin 17 vaccine--Aphton: Anti-gastrin 17 immunogen, G17DT.
, 2003
)
2.48
"Gastrin 17 (G17) is a potent stimulant of gastric acid secretion in vivo. "( The effects of various gastrins on intracellular free Ca2+ in isolated pig parietal cells.
Cabero, JL; Mårdh, S; Rehfeld, JF, 1989
)
1.72

Effects

Gastrin 17 (G-17) has been proposed as a non-invasive marker of GERD. This is due to the negative feedback between acid secretion and this hormone.

ExcerptReferenceRelevance
"Gastrin 17 (G-17) has been proposed to be related with GERD, due to the negative feedback between acid secretion and this hormone."( Low Levels of Gastrin 17 are Related with Endoscopic Findings of Esophagitis and Typical Symptoms of GERD.
Antico, A; Baldassarre, G; Barchi, A; Crafa, P; De Bortoli, N; Di Mario, F; Ferronato, A; Franceschi, M; Franzoni, L; Ghisa, M; Panozzo, MP; Rodriguez-Castro, K; Russo, M; Savarino, E, 2021
)
1.7
"Gastrin 17 (G-17) has been proposed as a non-invasive marker of GERD, due to the negative feedback between acid and the hormone."( Diagnosis of GERD in typical and atypical manifestations.
Barchi, A; Cesario, S; De' Angelis, GL; Di Mario, F; Leandro, G; Meschi, T; Miraglia, C; Nouvenne, A; Scida, S, 2018
)
1.2

Compound-Compound Interactions

ExcerptReferenceRelevance
"To explore the value of the Helicobacter pylori test in combination with the determination of plasma pepsinogen (PG) and gastrin 17 in screening the precancerous status of gastric cancer and gastric cancer in the healthy population, between 2019 and 2022, we enrolled a total of 402 subjects who went to the physical examination in the Center of Health Management of Ganzhou people's Hospital and additionally underwent the urea (14C) breath test and determination of PGI, PGII and G-17."( Analysis of the Value of Helicobacter pylori Test in Combination with the Determination of Plasma Propepsin and Gastrin 17 in Screening the Precancerous Status of Gastric Cancer.
Chen, X; Liao, G; Liu, M; Xiao, M; Zhang, Z, 2022
)
1.14

Dosage Studied

ExcerptRelevanceReference
" Dose-response studies were performed using intravenous histamine or tetragastrin."( Stimulation of gastric acid secretion in the rhesus monkey.
Harmon, JW; Trout, HH; Zinner, M, 1985
)
0.27
" The span of the dose-response curves was wide, suggesting the existence of receptor heterogeneity."( Receptors on smooth muscle cells: characterization by contraction and specific antagonists.
Bitar, KN; Makhlouf, GM, 1982
)
0.26
" During the third hour of prolonged intravenous infusions of G34 and G17, the exogenous dosage of G34 required to produce the same blood concentration of gastrin was only one-fourth that of G17."( Similar acid stimulatory potencies of synthetic human big and little gastrins in man.
Eysselein, VE; Maxwell, V; Reedy, T; Walsh, JH; Wünsch, E, 1984
)
0.27
" Similar effects were observed on guinea-pig "in vitro" stomach preparation where PM2 and Papaverine were ineffective in modifying Histamine dose-response curves and PM3 reduced significantly maximal peak effects of Histamine, behaving as a non-competitive antagonist."( [Pharmacological actions of alkylaminoalkyl-phenylbenzisothazole compounds on the gastrointestinal tract].
Barocelli, E; Bordi, F; Chiavarini, M; Impicciatore, M; Morini, G; Plazzi, P, 1984
)
0.27
" The dose-response curve for CCK-8 alone to induce gallbladder contraction was not significantly different from those caused by CCK-8 plus 1 mumol/L tetrodotoxin or 1 mumol/L atropine."( Characterization of cholecystokinin receptors on the human gallbladder.
Coleman, R; Concepcion, W; Cox, KL; Esquivel, CO; Nakazato, P; Tokunaga, Y, 1993
)
0.29
" To further evaluate the role of cholecystokinin (CCK) in regulating acid output in humans, dose-response curves were constructed to CCK8 or G17 (6."( Cholecystokinin is a physiological regulator of gastric acid secretion in man.
Aufderhaar, U; Bauerfeind, P; Beglinger, C; Burckhardt, B; Delco, F; Ensinck, JW; Gyr, K; Ketterer, S; Meier, R, 1994
)
0.29
" Dose-response experiments revealed the following potencies for SOM secretion: G-17s = CCK-8s > G-17 ns >> CCK-8ns."( Cholecystokinin (CCK) regulates somatostatin secretion through both the CCK-A and CCK-B/gastrin receptors in sheep.
Shulkes, A; Zavros, Y, 1997
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
gastrinA family of gastrointestinal peptide hormones that stimulate the secretion of gastric acid. Gastrin is found primarily in three forms: gastrin-34 ('big gastrin'), gastrin-17 ('little gastrin') and gastrin-14 ('minigastrin').
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cholecystokinin receptor type AHomo sapiens (human)IC50 (µMol)0.85110.00010.30381.9000AID1572001
Gastrin/cholecystokinin type B receptorHomo sapiens (human)IC50 (µMol)0.00410.00010.36154.0000AID1572002
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cholecystokinin receptor type AHomo sapiens (human)EC50 (µMol)0.26910.00000.05050.2691AID1572003
Gastrin/cholecystokinin type B receptorHomo sapiens (human)EC50 (µMol)0.00050.00000.00850.0270AID1572004
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (15)

Processvia Protein(s)Taxonomy
neuron migrationCholecystokinin receptor type AHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayCholecystokinin receptor type AHomo sapiens (human)
axonogenesisCholecystokinin receptor type AHomo sapiens (human)
forebrain developmentCholecystokinin receptor type AHomo sapiens (human)
cholecystokinin signaling pathwayCholecystokinin receptor type AHomo sapiens (human)
G protein-coupled receptor signaling pathwayCholecystokinin receptor type AHomo sapiens (human)
cellular response to hormone stimulusCholecystokinin receptor type AHomo sapiens (human)
regulation of hormone secretionCholecystokinin receptor type AHomo sapiens (human)
gastric acid secretionGastrin/cholecystokinin type B receptorHomo sapiens (human)
cell surface receptor signaling pathwayGastrin/cholecystokinin type B receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayGastrin/cholecystokinin type B receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationGastrin/cholecystokinin type B receptorHomo sapiens (human)
positive regulation of cell population proliferationGastrin/cholecystokinin type B receptorHomo sapiens (human)
cholecystokinin signaling pathwayGastrin/cholecystokinin type B receptorHomo sapiens (human)
pH reductionGastrin/cholecystokinin type B receptorHomo sapiens (human)
digestive tract developmentGastrin/cholecystokinin type B receptorHomo sapiens (human)
gland developmentGastrin/cholecystokinin type B receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
cholecystokinin receptor activityCholecystokinin receptor type AHomo sapiens (human)
peptide hormone bindingCholecystokinin receptor type AHomo sapiens (human)
peptide bindingCholecystokinin receptor type AHomo sapiens (human)
cholecystokinin receptor activityGastrin/cholecystokinin type B receptorHomo sapiens (human)
protein bindingGastrin/cholecystokinin type B receptorHomo sapiens (human)
gastrin receptor activityGastrin/cholecystokinin type B receptorHomo sapiens (human)
peptide hormone bindingGastrin/cholecystokinin type B receptorHomo sapiens (human)
type B gastrin/cholecystokinin receptor bindingGastrin/cholecystokinin type B receptorHomo sapiens (human)
1-phosphatidylinositol-3-kinase regulator activityGastrin/cholecystokinin type B receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
nucleoplasmCholecystokinin receptor type AHomo sapiens (human)
cytosolCholecystokinin receptor type AHomo sapiens (human)
plasma membraneCholecystokinin receptor type AHomo sapiens (human)
membraneCholecystokinin receptor type AHomo sapiens (human)
plasma membraneCholecystokinin receptor type AHomo sapiens (human)
plasma membraneGastrin/cholecystokinin type B receptorHomo sapiens (human)
intracellular membrane-bounded organelleGastrin/cholecystokinin type B receptorHomo sapiens (human)
plasma membraneGastrin/cholecystokinin type B receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID1572002Displacement of [125I]-CCK-8 from human CCK2R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Structure-Activity Relationships and Characterization of Highly Selective, Long-Acting, Peptide-Based Cholecystokinin 1 Receptor Agonists.
AID1572003Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Structure-Activity Relationships and Characterization of Highly Selective, Long-Acting, Peptide-Based Cholecystokinin 1 Receptor Agonists.
AID1572001Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Structure-Activity Relationships and Characterization of Highly Selective, Long-Acting, Peptide-Based Cholecystokinin 1 Receptor Agonists.
AID1572004Agonist activity at human CCK2R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Structure-Activity Relationships and Characterization of Highly Selective, Long-Acting, Peptide-Based Cholecystokinin 1 Receptor Agonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (395)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990101 (25.57)18.7374
1990's84 (21.27)18.2507
2000's116 (29.37)29.6817
2010's72 (18.23)24.3611
2020's22 (5.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 34.20

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index34.20 (24.57)
Research Supply Index6.08 (2.92)
Research Growth Index4.52 (4.65)
Search Engine Demand Index48.33 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (34.20)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials22 (5.34%)5.53%
Reviews17 (4.13%)6.00%
Case Studies1 (0.24%)4.05%
Observational2 (0.49%)0.25%
Other370 (89.81%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]