ArticleBritish journal of pharmacology2010
The proton-coupled amino acid transporter, SLC36A1 (hPAT1), transports Gly-Gly, Gly-Sar and other Gly-Gly mimetics.
Article in British journal of pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 33 citations in OpenAlex.
- Exploring Vitamin D Signaling-Associated Biomarkers and Their Diagnostic Value in Diabetic Retinopathy: A Combined Transcriptomic and Single-Cell Analysis With Experimental Validation.Journal of diabetes research · 2026Article
- Non-Steroidal Anti-Inflammatory Drugs Are Inhibitors of the Intestinal Proton-Coupled Amino Acid Transporter (PAT1): Ibuprofen and Diclofenac Are Non-Translocated Inhibitors.Pharmaceutics · 2025Article
- Functional Characterization of the Lysosomal Peptide/Histidine Transporter PHT1 (Biomolecules · 2024Article
- Effects of glutamine, glutamate, and aspartate on intestinal barrier integrity and amino acid pool of the small intestine in piglets with normal or low energy diet.Frontiers in veterinary science · 2023Article
- Interactions of Betel Quid Constituents with Drug Disposition Pathways: An Overview.Current drug metabolism · 2023Article
- SNAT2 is responsible for hyperosmotic induced sarcosine and glycine uptake in human prostate PC-3 cells.Pflugers Archiv : European journal of physiology · 2022Article
- Diet evolution of carnivorous and herbivorous mammals in Laurasiatheria.BMC ecology and evolution · 2022Article
- Insulin stimulates β-alanine uptake in skeletal muscle cells in vitro.Amino acids · 2021Article
- Rapid and Sensitive Quantification of Intracellular Glycyl-Sarcosine for Semi-High-Throughput Screening for Inhibitors of PEPT-1.Pharmaceutics · 2021Article
- Molecular phyloecology suggests a trophic shift concurrent with the evolution of the first birds.Communications biology · 2021Article
- Zwitterionic micelles efficiently deliver oral insulin without opening tight junctions.Nature nanotechnology · 2020Article
- Lysosomal recycling of amino acids affects ER quality control.Science advances · 2020Article
- Solvent effects on the structures and vibrational features of zwitterionic dipeptides: L-diglycine and L-dialanine.Journal of molecular modeling · 2015Article
- Sertraline inhibits the transport of PAT1 substrates in vivo and in vitro.British journal of pharmacology · 2013Article
- Comparative digestive physiology.Comprehensive Physiology · 2013Review
- Function and expression of the proton-coupled amino acid transporter PAT1 along the rat gastrointestinal tract: implications for intestinal absorption of gaboxadol.British journal of pharmacology · 2012Article
- Rectal absorption of vigabatrin, a substrate of the proton coupled amino acid transporter (PAT1, Slc36a1), in rats.Pharmaceutical research · 2012Article
- Dipeptide forms of glycine support mouse preimplantation embryo development in vitro and provide protection against high media osmolality.Journal of assisted reproduction and genetics · 2012Article
- A novel fungal family of oligopeptide transporters identified by functional metatranscriptomics of soil eukaryotes.The ISME journal · 2011Article
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND AND PURPOSE The intestinal proton-coupled amino acid transporter, SLC36A1, transports zwitterionic α-amino acids and drugs such as vigabatrin, gaboxadol and δ-aminolevulinic acid. We hypothesize that SLC36A1 might also transport some dipeptides. The aim of the present study was to investigate SLC36A1-mediated transport of Gly-Gly and Gly-Gly mimetics, and to investigate Gly-Sar transport via SLC36A1 and the proton-coupled dipeptide/tripeptide transporter, SLC15A1 in Caco-2 cells. EXPERIMENTAL APPROACH Transport of a compound via SLC36A1 was determined by its ability to induce an increase in the inward current of two-electrode voltage clamped SLC36A1 cRNA-injected Xenopus laevis oocytes. SLC36A1-mediated L-[³H]Pro uptake in Caco-2 cells was measured in the absence and presence of Gly-Gly or Gly-Sar. In addition, apical [¹⁴C]Gly-Sar uptake was measured in the absence and presence of the SLC36A1 inhibitor 5-hydroxy-L-tryptophan (5-HTP) or the SLC15A1 inhibitor L-4,4'-biphenylalanyl-L-proline (Bip-Pro). KEY RESULTS In SLC36A1-expressing oocytes, an inward current was induced by Gly-Sar, Gly-Gly, δ-aminolevulinic acid, β-aminoethylglycine, δ-aminopentanoic acid, GABA, Gly and Pro, whereas Val, Leu, mannitol, 5-HTP and the dipeptides Gly-Ala, Gly-Pro and Gly-Phe did not evoke currents. In Caco-2 cell monolayers, the apical uptake of 30 mM Gly-Sar was inhibited by 20 and 22% in the presence of 5-HTP or Bip-Pro, respectively, and by 48% in the presence of both. CONCLUSION AND IMPLICATIONS Our results suggest that whereas Gly-Gly amid bond bioisosteres are widely accepted by the hPAT1 carrier, dipeptides in general are not; and therefore, Gly-Sar might structurally define the size limit of dipeptide transport via SLC36A1.
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