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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
2005-6-28
pubmed:abstractText
Human proton-dependent peptide transporters, PEPT1 and PEPT2, mediate the cellular uptake of di- and tripeptides as well as a variety of drug molecules. Although PEPT1 and PEPT2 have been cloned from many species, there are no data available for monkey, an important pharmacological and preclinical species in drug development. In this study, it was first verified that monkey intestine transports a model dipeptide, Gly-Sar, in a proton-dependent manner (0.30 +/- 0.05 pmol cm(-2) s(-1) at pH 6.0 and 0.10 +/- 0.03 pmol cm(-2) s(-1) at pH 7.4) in the absorptive direction, presumably by monkey PEPT1. RT-PCR and rapid amplification of cDNA ends (RACE) were then used to clone monkey PEPT1 and PEPT2. Monkey PEPT1 (2127 bp and 708 amino acids) was found to be >94 and > 92% identical to human PEPT1 at the cDNA and amino acid level, respectively. Monkey PEPT2 (2190 bp and 729 amino acids) was found to be > 97% identical to human PEPT2 at both the cDNA and amino acid levels. Functional comparison of human and monkey peptide transporters expressed in HeLa cells suggested that functionalities of PEPT1 and PEPT2 were largely conserved in terms of Gly-Sar uptake kinetics and inhibitor specificity (for most tested substrates). Finally, Northern and RT-PCR analyses revealed some differences in tissue mRNA levels of peptide transporters between human and monkey.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
1543-8384
pubmed:author
pubmed:issnType
Print
pubmed:volume
1
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
201-10
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:articleTitle
Comparison of human and monkey peptide transporters: PEPT1 and PEPT2.
pubmed:affiliation
Drug Disposition, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA.
pubmed:publicationType
Journal Article, Comparative Study