PMID: 11901210Mar 20, 2002Paper

Transport of amino acid-related compounds mediated by L-type amino acid transporter 1 (LAT1): insights into the mechanisms of substrate recognition

Molecular Pharmacology
Hiroshi UchinoHitoshi Endou

Abstract

The L-type amino acid transporter 1 (LAT1) is an Na(+)-independent neutral amino acid transporter subserving the amino acid transport system L. Because of its broad substrate selectivity, system L has been proposed to be responsible for the permeation of amino acid-related drugs through the plasma membrane. To understand the mechanisms of substrate recognition, we have examined the LAT1-mediated transport using a Xenopus laevis oocyte expression system. LAT1-mediated [(14)C]phenylalanine uptake was strongly inhibited in a competitive manner by aromatic-amino acid derivatives including L-dopa, alpha-methyldopa, melphalan, triiodothyronine, and thyroxine, whereas phenylalanine methyl ester, N-methyl phenylalanine, dopamine, tyramine, carbidopa, and droxidopa did not inhibit [(14)C]phenylalanine uptake. Gabapentin, a gamma-amino acid, also exerted a competitive inhibition on LAT1-mediated [(14)C]phenylalanine uptake. Although most of the compounds that inhibited LAT1-mediated uptake were able to induce the efflux of [(14)C]phenylalanine preloaded to the oocytes expressing LAT1 through the obligatory exchange mechanism, melphalan, triiodothyronine, and thyroxine did not induce the significant efflux. Based on the experimental and s...Continue Reading

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Citations

Jun 8, 2011·Amino Acids·Nobuhiro KawaiEiji Shimizu
Jul 2, 2009·Pharmaceutical Research·Ken-ichi Hosoya, Masanori Tachikawa
Apr 10, 2013·Biochemical Pharmacology·David DickensMunir Pirmohamed
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Nov 5, 2008·Biological & Pharmaceutical Bulletin·Ken-Ichi HosoyaMasanori Tachikawa
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