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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
|
pubmed:dateCreated |
1985-4-12
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pubmed:abstractText |
A series of tri- and tetrapeptide derivatives, analogues of the gastrin C-terminal region with no phenylalanine residue, were synthesized. These peptides were tested for their ability to inhibit gastrin-stimulated acid secretion in vivo as well as binding of [125I]-(Nle11)-HG-13 to gastric mucosal cell receptors in vitro. Most of the peptides tested exhibited gastrin antagonist activity in vivo and in vitro. Most active derivatives were 20-30 times more potent than the well-known gastrin antagonist derivatives proglumide and benzotript and had 20-200 times more binding affinity. The smallest fragment exhibiting antagonist activity was the tripeptide Boc-L-tryptophyl-L-methionyl-L-aspartic acid amide.
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pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Mar
|
pubmed:issn |
0022-2623
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
28
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
273-8
|
pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:3973899-Animals,
pubmed-meshheading:3973899-Chemical Phenomena,
pubmed-meshheading:3973899-Chemistry,
pubmed-meshheading:3973899-Gastric Acid,
pubmed-meshheading:3973899-Gastrins,
pubmed-meshheading:3973899-Oligopeptides,
pubmed-meshheading:3973899-Peptide Fragments,
pubmed-meshheading:3973899-Rats,
pubmed-meshheading:3973899-Structure-Activity Relationship
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pubmed:year |
1985
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pubmed:articleTitle |
Structure-activity relationships of C-terminal tri- and tetrapeptide fragments that inhibit gastrin activity.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|