ArticleMolecular pharmaceutics2013
Polyamine transport by the polyspecific organic cation transporters OCT1, OCT2, and OCT3.
Article in Molecular pharmaceutics, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 53 papers, 1 of them a synthesis that pooled it.
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Who cites it
53 citing papers in PubMed, 1 synthesis or guideline pooled it, 86 citations in OpenAlex.
- Identification of Novel Intronic SNPs in Transporter Genes Associated with Metformin Side Effects.Genes · 2023Pooled it
- Functional Characterization of the P-Type ATPases ATP13A3 and ATP13A4 as Plasma Membrane Polyamine Transporters.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2026Article
- Spermidine in the aging brain: mechanisms, preclinical evidence, and clinical perspectives.Molecular biology reports · 2026Review
- Polyamine metabolism in cancer: drivers of immune evasion, ferroptosis and therapy resistance.Expert reviews in molecular medicine · 2025Review
- Age-Dependent Redistribution of the Life-Important Enzyme in the Retina: Adult Müller Glial Cells' Endfeet Lack Spermine Synthase Expression.Biomolecules · 2025Article
- Transport of Small Aliphatic Amines by Polyspecific Solute Carriers: Deciphering Structure-Function Relationships.ACS pharmacology & translational science · 2025Article
- Transcriptomic Analysis Reveals the Mechanisms of Cadmium Transport and Detoxification in Portuguese Oysters (Animals : an open access journal from MDPI · 2025Article
- Spermidine Synthase Localization in Retinal Layers: Early Age Changes.International journal of molecular sciences · 2024Article
- Interaction and Transport of Benzalkonium Chlorides by the Organic Cation and Multidrug and Toxin Extrusion Transporters.Drug metabolism and disposition: the biological fate of chemicals · 2024Article
- The efflux pumps Rv1877 and Rv0191 play differential roles in the protection ofFrontiers in microbiology · 2024Article
- Polyamines: Key Players in Immunometabolism and Immune Regulation.Journal of cellular immunology · 2024Article
- Involvement of mammalian SoLute Carriers (SLC) in the traffic of polyamines.Frontiers in molecular biosciences · 2024Review
- The Molecular Role of Polyamines in Age-Related Diseases: An Update.International journal of molecular sciences · 2023Review
- Inhibition of nicotinic acetylcholine receptors by oligoarginine peptides and polyamine-related compounds.Frontiers in pharmacology · 2023Article
- The Polyamine Spermine Potentiates the Propagation of Negatively Charged Molecules through the Astrocytic Syncytium.Biomolecules · 2022Article
- Multigenerational Exposure to Uranium Changes Sperm Metabolome in Rats.International journal of molecular sciences · 2022Article
- Interrogation of T Cell-Enriched Tumors Reveals Prognostic and Immunotherapeutic Implications of Polyamine Metabolism.Cancer research communications · 2022Article
- Polyamines protect boar sperm from oxidative stress in vitro.Journal of animal science · 2022Article
- Unique Chemistry, Intake, and Metabolism of Polyamines in the Central Nervous System (CNS) and Its Body.Biomolecules · 2022Review
- Polyamine Immunometabolism: Central Regulators of Inflammation, Cancer and Autoimmunity.Cells · 2022Review
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
Polyamines are ubiquitous organic cations implicated in many physiological processes. Because they are positively charged at physiological pH, carrier-mediated systems are necessary for effective membrane permeation, but the identity of specific polyamine transporter proteins in eukaryotic cells remains unclear. Polyspecific organic cation transporters (OCTs) interact with many natural and xenobiotic monovalent cations and have been reported to transport dicationic compounds, including the short polyamine putrescine. In this study, we used Xenopus oocytes expressing mammalian OCT1 (SLC22A1), OCT2 (SLC22A2), or OCT3 (SLC22A3) to assess binding and transport of longer-chain polyvalent polyamines. In OCT-expressing oocytes, [(3)H]MPP(+) uptake rates were 15- to 35-fold higher than in noninjected oocytes, whereas those for [(3)H]spermidine increased more modestly above the background, up to 3-fold. This reflected up to 20-fold lower affinity for spermidine than for MPP(+); thus, K(0.5) for MPP(+) was ~50 μM in OCT1, ~170 μM in OCT2, and ~60 μM in OCT3, whereas for spermidine, K(0.5) was ~1 mM in OCT1, OCT2, and OCT3. J(max) values for MPP(+) and spermidine were within the same range, suggesting that both compounds are transported at a similar turnover rate. To gain further insight into OCT substrate specificity, we screened a selection of structural polyamine analogues for effect on [(3)H]MPP(+) uptake. In general, blocking potency increased with overall hydrophobic character, which indicates that, as for monovalent cations, hydrophobicity is a major requirement for recognition in polyvalent OCT substrates and inhibitors. Our results demonstrate that the natural polyamines are low affinity, but relatively high turnover, substrates for OCTs. The identification of OCTs as polyamine transport systems may contribute to further understanding of the mechanisms involved in polyamine homeostasis and aid in the design of polyamine-like OCT-targeted drugs.
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