ArticleBritish journal of pharmacology2010
Delta-aminolevulinic acid is a substrate for the amino acid transporter SLC36A1 (hPAT1).
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 21 papers.
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Who cites it
21 citing papers in PubMed, 49 citations in OpenAlex.
- 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
- Exploring Amino Acid Transporters as Therapeutic Targets for Cancer: An Examination of Inhibitor Structures, Selectivity Issues, and Discovery Approaches.Pharmaceutics · 2024Review
- SNAT2 is responsible for hyperosmotic induced sarcosine and glycine uptake in human prostate PC-3 cells.Pflugers Archiv : European journal of physiology · 2022Article
- A Recap of Heme Metabolism towards Understanding Protoporphyrin IX Selectivity in Cancer Cells.International journal of molecular sciences · 2022Review
- Detection of Canine Urothelial Carcinoma Cells in Urine Using 5-Aminolevulinic Acid.Animals : an open access journal from MDPI · 2022Article
- Mechanisms of Neuronal Damage in Acute Hepatic Porphyrias.Diagnostics (Basel, Switzerland) · 2021Review
- Key transporters leading to specific protoporphyrin IX accumulation in cancer cell following administration of aminolevulinic acid in photodynamic therapy/diagnosis.International journal of clinical oncology · 2021Review
- Porphyric Neuropathy: Pathophysiology, Diagnosis, and Updated Management.Current neurology and neuroscience reports · 2020Review
- Blood-Brain Barrier, Blood-Brain Tumor Barrier, and Fluorescence-Guided Neurosurgical Oncology: Delivering Optical Labels to Brain Tumors.Frontiers in oncology · 2020Review
- Mechanistic study of PpIX accumulation using the JFCR39 cell panel revealed a role for dynamin 2-mediated exocytosis.Scientific reports · 2019Article
- Dynamics of absorption, metabolism, and excretion of 5-aminolevulinic acid in human intestinal Caco-2 cells.Biochemistry and biophysics reports · 2017Article
- The proton-coupled oligopeptide transporter 1 plays a major role in the intestinal permeability and absorption of 5-aminolevulinic acid.British journal of pharmacology · 2016Article
- In vivo and in vitro evaluations of intestinal gabapentin absorption: effect of dose and inhibitors on carrier-mediated transport.Pharmaceutical research · 2015Article
- Sertraline inhibits the transport of PAT1 substrates in vivo and in vitro.British journal of pharmacology · 2013Article
- 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
- δ-Aminolevulinic acid and its methyl ester induce the formation of Protoporphyrin IX in cultured sensory neurones.Naunyn-Schmiedeberg's archives of pharmacology · 2011Article
- SLC36A4 (hPAT4) is a high affinity amino acid transporter when expressed in Xenopus laevis oocytes.The Journal of biological chemistry · 2011Article
- Ibuprofen is a non-competitive inhibitor of the peptide transporter hPEPT1 (SLC15A1): possible interactions between hPEPT1 substrates and ibuprofen.British journal of pharmacology · 2010Article
- Intracellular amino acid sensing and mTORC1-regulated growth: new ways to block an old target?Current opinion in investigational drugs (London, England : 2000) · 2010Review
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposedelta-Aminolevulinic acid (ALA) is used in cancer patients for photodynamic diagnosis or therapy. Oral administration of ALA has been used in patients with prostate and bladder cancer. The present aim was to investigate the mechanism of intestinal absorption of ALA and its transport via the amino acid transporter SLC36A1. EXPERIMENTAL APPROACH: In vitro investigations of ALA affinity for and uptake via SLC36A1 and SLC15A1 were performed in Caco-2 cell monolayers. Interaction of ALA with SLC15A1 was investigated in MDCK/SLC15A1 cells, whereas interactions with SLC36A1 were investigated in COS-7 cells transiently expressing SLC36A1. KEY
resultsALA inhibited SLC36A1-mediated L-[(3)H]Pro and SLC15A1-mediated [(14)C]Gly-Sar uptake in Caco-2 cell monolayers with IC(50) values of 11.3 and 2.1 mM respectively. In SLC36A1-expressing COS-7 cells, the uptake of [(14)C]ALA was saturable with a K(m) value of 6.8 +/- 3.0 mM and a V(max) of 96 +/- 13 pmol x cm(-2) x min(-1). Uptake of [(14)C]ALA was pH and concentration dependent, and could be inhibited by glycine, proline and GABA. In a membrane potential assay, translocation of ALA via SLC36A1 was concentration dependent, with a K(m) value of 3.8 +/- 1.0 mM. ALA is thus a substrate for SLC36A1. In Caco-2 cells, apical [(14)C]ALA uptake was pH dependent, but Na(+) independent, and completely inhibited by 5-hydroxy-L-tryptophan and L-4,4'-biphenylalanyl-l-proline. CONCLUSIONS AND IMPLICATIONS. ALA was a substrate for SLC36A1, and the apical absorption in Caco-2 cell was only mediated by SLC36A1 and SLC15A1. This advances our understanding of intestinal absorption mechanisms of ALA, as well as its potential for drug interactions.
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