Linked Life Data

14706811

Source:http://linkedlifedata.com/resource/pubmed/id/14706811

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
2004-1-6
pubmed:abstractText
Peptide transporter 1, PEPT1, of the mammalian enterocyte is presently under intense investigation in many laboratories because of its nutritional importance in the absorption of protein hydrolysis products and because more recent studies have shown that many drugs and prodrugs gain entry into the systemic circulation via PEPT1. Until the exact structural features of the substrate binding site of PEPT1 become available, for example by X-ray crystallography, determination of affinities followed by proof of actual membrane translocation will have to suffice when testing for possible new substrates for PEPT1. Affinity constants reflect the strength of their interaction with the binding site of the transporter. A review of the literature shows a wide range of affinity constants between 2 microM and 30 mM. We consider affinity constants for substrates or inhibitors of PEPT1 lower than 0.5 mM as high affinity, between 0.5 and 5.0 mM as medium affinity and above 5 mM as low affinity. Values above 15 mM we consider with great caution. In this mini-review we discuss affinities and structural determinants which affect affinities of a variety of substrates for PEPT1.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
0928-0987
pubmed:author
pubmed:issnType
Print
pubmed:volume
21
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
53-60
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
2004
pubmed:articleTitle
The intestinal H+/peptide symporter PEPT1: structure-affinity relationships.
pubmed:affiliation
Membrane Transport Group, Biozentrum of Martin-Luther-University Halle-Wittenberg, Weinbergweg 22, D-06120 Halle, Germany. brandsch@biozentrum.uni-halle.de
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Review, Research Support, Non-U.S. Gov't