Source:http://linkedlifedata.com/resource/pubmed/id/20862774
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2011-1-4
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pubmed:abstractText |
The purpose of this study was to determine the relative importance of peptide transporter 1 (PEPT1) in the uptake of peptides/mimetics from mouse small intestine, using glycylsarcosine (GlySar). After isolating jejunal tissue from wild-type and Pept1 null mice, 2 cm intestinal segments were everted and mounted on glass rods for tissue uptake studies. [(14)C]GlySar (4 ?M) was studied as a function of time, temperature, sodium and pH, concentration, and potential inhibitors. Compared with wild-type animals, Pept1 null mice exhibited a 78% reduction in GlySar uptake at pH 6.0 at 37°C. GlySar uptake showed pH dependence, with peak values between pH 6.0 and 6.5 in wild-type animals, whereas no such tendency was observed in Pept1 null mice. GlySar exhibited Michaelis-Menten uptake kinetics and a minor nonsaturable component in wild-type animals. In contrast, GlySar uptake occurred only by a nonsaturable process in Pept1 null mice. GlySar uptake was significantly inhibited by dipeptides, aminocephalosporins, angiotensin-converting enzyme inhibitors, and the antiviral prodrug valacyclovir; these inhibitors had little, if any, effect on the uptake of GlySar in Pept1 null mice. The findings demonstrate that PEPT1 plays a critical role in the uptake of GlySar in jejunum and suggest that PEPT1 is the major transporter responsible for the intestinal absorption of small peptides.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Dipeptides,
http://linkedlifedata.com/resource/pubmed/chemical/Slc15a1 protein, mouse,
http://linkedlifedata.com/resource/pubmed/chemical/Sodium,
http://linkedlifedata.com/resource/pubmed/chemical/Symporters,
http://linkedlifedata.com/resource/pubmed/chemical/glycylsarcosine
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
1520-6017
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pubmed:author | |
pubmed:copyrightInfo |
Copyright © 2010 Wiley-Liss, Inc.
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pubmed:issnType |
Electronic
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pubmed:volume |
100
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
767-74
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pubmed:meshHeading |
pubmed-meshheading:20862774-Animals,
pubmed-meshheading:20862774-Dipeptides,
pubmed-meshheading:20862774-Hydrogen-Ion Concentration,
pubmed-meshheading:20862774-Jejunum,
pubmed-meshheading:20862774-Kinetics,
pubmed-meshheading:20862774-Mice,
pubmed-meshheading:20862774-Mice, Inbred C57BL,
pubmed-meshheading:20862774-Mice, Knockout,
pubmed-meshheading:20862774-Sodium,
pubmed-meshheading:20862774-Symporters,
pubmed-meshheading:20862774-Temperature
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pubmed:year |
2011
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pubmed:articleTitle |
Peptide transporter 1 is responsible for intestinal uptake of the dipeptide glycylsarcosine: studies in everted jejunal rings from wild-type and Pept1 null mice.
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pubmed:affiliation |
Department of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109, USA.
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pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
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