ArticleMolecular pharmaceutics2011
OCT2 and MATE1 provide bidirectional agmatine transport.
Article in Molecular pharmaceutics, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 66 citations in OpenAlex.
- Agmatine induces mitophagy via the PTS-I2R pathway to increase autophagic flux and attenuate sepsis-induced intestinal epithelial cell apoptosis.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2026Article
- Transport of Small Aliphatic Amines by Polyspecific Solute Carriers: Deciphering Structure-Function Relationships.ACS pharmacology & translational science · 2025Article
- The role of polyamine metabolism in cellular function and physiology.American journal of physiology. Cell physiology · 2024Review
- Insights into the action of the pharmaceutical metformin: Targeted inhibition of the gut microbial enzyme agmatinase.iScience · 2024Article
- Involvement of mammalian SoLute Carriers (SLC) in the traffic of polyamines.Frontiers in molecular biosciences · 2024Review
- Biodistribution of Agmatine to Brain and Spinal Cord after Systemic Delivery.The Journal of pharmacology and experimental therapeutics · 2023Article
- Polyamines and Their Metabolism: From the Maintenance of Physiological Homeostasis to the Mediation of Disease.Medical sciences (Basel, Switzerland) · 2022Review
- Interrogation of T Cell-Enriched Tumors Reveals Prognostic and Immunotherapeutic Implications of Polyamine Metabolism.Cancer research communications · 2022Article
- The Interplay between Uremic Toxins and Albumin, Membrane Transporters and Drug Interaction.Toxins · 2022Review
- Substrate-DependentInternational journal of molecular sciences · 2021Article
- Article
- Interactions of Environmental Chemicals and Natural Products With ABC and SLC Transporters in the Digestive System of Aquatic Organisms.Frontiers in physiology · 2021Article
- Substrates and Inhibitors of Organic Cation Transporters (OCTs) and Plasma Membrane Monoamine Transporter (PMAT) and Therapeutic Implications.Handbook of experimental pharmacology · 2021Article
- The Role of Mitochondria in Drug-Induced Kidney Injury.Frontiers in physiology · 2020Review
- Dietary and Gut Microbiota Polyamines in Obesity- and Age-Related Diseases.Frontiers in nutrition · 2019Review
- What We Know and What We Need to Know about Aromatic and Cationic Biogenic Amines in the Gastrointestinal Tract.Foods (Basel, Switzerland) · 2018Review
- Evaluation of Polyamine Transport Inhibitors in a Drosophila Epithelial Model Suggests the Existence of Multiple Transport Systems.Medical sciences (Basel, Switzerland) · 2017Article
- Incorporation of a Biguanide Scaffold Enhances Drug Uptake by Organic Cation Transporters 1 and 2.Molecular pharmaceutics · 2017Article
- Renal Drug Transporters and Drug Interactions.Clinical pharmacokinetics · 2017Review
- Phylogenetic, syntenic, and tissue expression analysis of slc22 genes in zebrafish (Danio rerio).BMC genomics · 2016Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Agmatine is a biogenic amine (l-arginine metabolite) of potential relevance to several central nervous system (CNS) conditions. The identities of transporters underlying agmatine and polyamine disposition in mammalian systems are not well-defined. The SLC-family organic cation transporters (OCT) OCT1 and OCT2 and multidrug and toxin extrusion transporter-1 (MATE1) are transport systems that may be of importance for the cellular disposition of agmatine and putrescine. We investigated the transport of [(3)H]agmatine and [(3)H]putrescine in human embryonic kidney (HEK293) cells stably transfected with hOCT1, hOCT2, and hMATE1. Agmatine transport by hOCT1 and hOCT2 was concentration-dependent, whereas only hOCT2 demonstrated pH-dependent transport. hOCT2 exhibited a greater affinity for agmatine (K(m) = 1.84 ± 0.38 mM) than did hOCT1 (K(m) = 18.73 ± 4.86 mM). Putrescine accumulation was pH- and concentration-dependent in hOCT2-HEK cells (K(m) = 11.29 ± 4.26 mM) but not hOCT1-HEK cells. Agmatine accumulation, in contrast to putrescine, was significantly enhanced by hMATE1 overexpression, and was saturable (K(m) = 240 ± 31 μM; V(max) = 192 ± 10 pmol/min/mg of protein). Intracellular agmatine was also trans-stimulated (effluxed) from hMATE1-HEK cells in the presence of an inward proton-gradient. The hMATE1-mediated transport of agmatine was inhibited by polyamines, the prototypical substrates MPP+ and paraquat, as well as guanidine and arcaine, but not l-arginine. These results suggest that agmatine disposition may be influenced by hOCT2 and hMATE1, two transporters critical in the renal elimination of xenobiotic compounds.
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