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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
201
pubmed:dateCreated
2010-11-24
pubmed:abstractText
Organic cation transporters (OCTs) of the solute carrier family (SLC) 22 and multidrug and toxin extrusion (MATE) transporters of the SLC47 family have been identified as uptake and efflux transporters, respectively, for xenobiotics including several clinically used drugs such as the antidiabetic agent metformin, the antiviral agent lamivudine, and the anticancer drug oxaliplatin. Expression of human OCT1 (SLC22A1) and OCT2 (SLC22A2) is highly restricted to the liver and kidney, respectively. By contrast, OCT3 (SLC22A3) is more widely distributed. MATEs (SLC47A1, SLC47A2) are predominantly expressed in human kidney. Data on in vitro studies reporting a large number of substrates and inhibitors of OCTs and MATEs are systematically summarized. Several genetic variants of human OCTs and in part of MATE1 have been reported, and some of them result in reduced in vitro transport activity corroborating data from studies with knockout mice. A comprehensive overview is given on currently known genotype-phenotype correlations for variants in OCTs and MATE1 related to protein expression, pharmacokinetics/-dynamics of transporter substrates, treatment outcome, and disease susceptibility.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0171-2004
pubmed:author
pubmed:issnType
Print
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
105-67
pubmed:dateRevised
2011-4-12
pubmed:meshHeading
pubmed:year
2011
pubmed:articleTitle
Organic cation transporters (OCTs, MATEs), in vitro and in vivo evidence for the importance in drug therapy.
pubmed:affiliation
Dr. Margarete Fischer-Bosch Institute of Clinical Pharmacology, Stuttgart, Germany. anne.nies@ikp-stuttgart.de
pubmed:publicationType
Journal Article, Review, Research Support, Non-U.S. Gov't