OCTN: A Small Transporter Subfamily with Great Relevance to Human Pathophysiology, Drug Discovery, and Diagnostics

Changing to a vegetarian diet reduces the body creatine pool in omnivorous women, but appears not to affect carnitine and carnosine homeostasis: a randomised trial

(2018) Laura Blancquaert et al.   BRITISH JOURNAL OF NUTRITION

Substrate Selectivity Check of the Ergothioneine Transporter

(2018) Julia Tschirka et al.   DRUG METABOLISM AND DISPOSITION

Recent advances in drug delivery via the organic cation/carnitine transporter 2 (OCTN2/SLC22A5)

(2018) Longfa Kou et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

SLC22A16 upregulation is an independent unfavorable prognostic indicator in gastric cancer

(2018) Wenhua Zhao et al.   Future Oncology

Cryo-EM structure of the human neutral amino acid transporter ASCT2

(2018) Alisa A. Garaeva et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Physiology of L-carnitine in plants in light of the knowledge in animals and microorganisms

(2018) Florian Jacques et al.   PLANT SCIENCE

Substrate-bound outward-open structure of a Na+-coupled sialic acid symporter reveals a new Na+ site

(2018) Weixiao Y. Wahlgren et al.   Nature Communications

Cryo-EM structure of the human neutral amino acid transporter ASCT2

(2018) Alisa A. Garaeva et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Pharmacogenetics of toxicity of 5-fluorouracil, doxorubicin and cyclophosphamide chemotherapy in breast cancer patients

(2018) Karolina Tecza et al.   Oncotarget

Characterization of Exosomal SLC22A5 (OCTN2) carnitine transporter

(2018) Lara Console et al.   Scientific Reports

CRISPR/Cas9 genome editing: Fueling the revolution in cancer immunotherapy

(2018) Xiaojun Liu et al.   Current Research in Translational Medicine

Enhanced expression of Organic Cation Transporters in bronchial epithelial cell layers following insults associated with asthma – Impact on salbutamol transport

(2017) Manali Mukherjee et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Beyond drug-drug interactions: effects of transporter inhibition on endobiotics, nutrients and toxins

(2017) Eve-Irene Lepist et al.   Expert Opinion on Drug Metabolism & Toxicology

Combination of l-Carnitine with Lipophilic Linkage-Donating Gemcitabine Derivatives as Intestinal Novel Organic Cation Transporter 2-Targeting Oral Prodrugs

(2017) Gang Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Acute Exercise Stimulates Carnitine Biosynthesis and OCTN2 Expression in Mouse Kidney

(2017) Tom L. Broderick et al.   KIDNEY & BLOOD PRESSURE RESEARCH

Impairment of the carnitine/organic cation transporter 1–ergothioneine axis is mediated by intestinal transporter dysfunction in chronic kidney disease

(2017) Yasuyuki Shinozaki et al.   KIDNEY INTERNATIONAL

Structure and allosteric inhibition of excitatory amino acid transporter 1

(2017) Juan C. Canul-Tec et al.   NATURE

Carnitine/Organic Cation Transporter OCTN1 Negatively Regulates Activation in Murine Cultured Microglial Cells

(2017) Takahiro Ishimoto et al.   NEUROCHEMICAL RESEARCH

l-Carnitine and Acetyl-l-carnitine Roles and Neuroprotection in Developing Brain

(2017) Gustavo C. Ferreira et al.   NEUROCHEMICAL RESEARCH

Glutamine Transport and Mitochondrial Metabolism in Cancer Cell Growth

(2017) Mariafrancesca Scalise et al.   Frontiers in Oncology

Plasma acylcarnitine concentrations reflect the acylcarnitine profile in cardiac tissues

(2017) Marina Makrecka-Kuka et al.   Scientific Reports

Multiple Drug Transporters Are Involved in Renal Secretion of Entecavir

(2016) Xi Yang et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Ergothioneine, an adaptive antioxidant for the protection of injured tissues? A hypothesis

(2016) Barry Halliwell et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Functional activity of L-carnitine transporters in human airway epithelial cells

(2016) Filippo Ingoglia et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Acetylcholine and acetylcarnitine transport in peritoneum: Role of the SLC22A4 (OCTN1) transporter

(2016) Lorena Pochini et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Carnitine transport and fatty acid oxidation

(2016) Nicola Longo et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Phylogenetic, syntenic, and tissue expression analysis of slc22 genes in zebrafish (Danio rerio)

(2016) Ivan Mihaljevic et al.   BMC GENOMICS

The complex metabolism of trimethylamine in humans: endogenous and exogenous sources

(2016) Jyoti Chhibber-Goel et al.   EXPERT REVIEWS IN MOLECULAR MEDICINE

Human macrophage differentiation induces OCTN2–mediated L-carnitine transport through stimulation of mTOR–STAT3 axis

(2016) Filippo Ingoglia et al.   JOURNAL OF LEUKOCYTE BIOLOGY

Transport of 3-fluoro-l-α-methyl-tyrosine (FAMT) by organic ion transporters explains renal background in [18F]FAMT positron emission tomography

(2016) Ling Wei et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

L503F variant of carnitine/organic cation transporter 1 efficiently transports metformin and other biguanides

(2016) Azusa Futatsugi et al.   JOURNAL OF PHARMACY AND PHARMACOLOGY

Identification and Characterization of Trimethylamine-N-oxide Uptake and Efflux Transporters

(2016) Wendy A. Teft et al.   MOLECULAR PHARMACEUTICS

X-ray structures and mechanism of the human serotonin transporter

(2016) Jonathan A. Coleman et al.   NATURE

Skeletal muscle mitochondria as a target to prevent or treat type 2 diabetes mellitus

(2016) Matthijs K. C. Hesselink et al.   Nature Reviews Endocrinology

Drosophila SLC22A Transporter Is a Memory Suppressor Gene that Influences Cholinergic Neurotransmission to the Mushroom Bodies

(2016) Yunchao Gai et al.   NEURON

The inhibitory effects of camptothecin (CPT) and its derivatives on the substrate uptakes mediated by human solute carrier transporters (SLCs)

(2016) Jian Zheng et al.   XENOBIOTICA

Muscle and liver-specific alterations in lipid and acylcarnitine metabolism after a single bout of exercise in mice

(2016) Miriam Hoene et al.   Scientific Reports

Food-derived hydrophilic antioxidant ergothioneine is distributed to the brain and exerts antidepressant effect in mice

(2016) Noritaka Nakamichi et al.   Brain and Behavior

Gene Ablation of Carnitine/Organic Cation Transporter 1 Reduces Gastrointestinal Absorption of 5-Aminosalicylate in Mice

(2015) Takuya Shimizu et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

Organic cation transporter Octn1-mediated uptake of food-derived antioxidant ergothioneine into infiltrating macrophages during intestinal inflammation in mice

(2015) Takuya Shimizu et al.   Drug Metabolism and Pharmacokinetics

Nuciferine restores potassium oxonate-induced hyperuricemia and kidney inflammation in mice

(2015) Ming-Xing Wang et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Immuno-detection of OCTN1 (SLC22A4) in HeLa cells and characterization of transport function

(2015) Lorena Pochini et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

Recent progress in revealing the biological and medical significance of the non-neuronal cholinergic system

(2015) Sergei A. Grando et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

Carnitine in bacterial physiology and metabolism

(2015) Jamie A. Meadows et al.   MICROBIOLOGY-SGM

Disorders of carnitine biosynthesis and transport

(2015) Ayman W. El-Hattab et al.   MOLECULAR GENETICS AND METABOLISM

The Prodrug Approach: A Successful Tool for Improving Drug Solubility

(2015) Daniela Jornada et al.   MOLECULES

Molecular basis of ligand recognition and transport by glucose transporters

(2015) Dong Deng et al.   NATURE

SLC38A9 is a component of the lysosomal amino acid sensing machinery that controls mTORC1

(2015) Manuele Rebsamen et al.   NATURE

The Phyre2 web portal for protein modeling, prediction and analysis

(2015) Lawrence A Kelley et al.   Nature Protocols

TMAO: A small molecule of great expectations

(2015) Marcin Ufnal et al.   NUTRITION

Effects of L-carnitine supplementation on respiratory distress syndrome development and prognosis in premature infants: A single blind randomized controlled trial

(2015) MEHMET ADNAN OZTURK et al.   Experimental and Therapeutic Medicine

The Poorly Membrane Permeable Antipsychotic Drugs Amisulpride and Sulpiride Are Substrates of the Organic Cation Transporters from the SLC22 Family

(2014) Joao N. Dos Santos Pereira et al.   AAPS Journal

Luteolin potentiates the sensitivity of colorectal cancer cell lines to oxaliplatin through the PPARγ/OCTN2 pathway

(2014) Qiang Qu et al.   ANTI-CANCER DRUGS

Non-neuronal cholinergic airway epithelium biology

(2014) Wolfgang Kummer et al.   CURRENT OPINION IN PHARMACOLOGY

l-Carnitine ester of prednisolone: Pharmacokinetic and pharmacodynamic evaluation of a type I prodrug

(2014) Jingxin Mo et al.   INTERNATIONAL JOURNAL OF PHARMACEUTICS

What do drug transporters really do?

(2014) Sanjay K. Nigam   NATURE REVIEWS DRUG DISCOVERY

Organic Cation Transporter-Mediated Ergothioneine Uptake in Mouse Neural Progenitor Cells Suppresses Proliferation and Promotes Differentiation into Neurons

(2014) Takahiro Ishimoto et al.   PLoS One

Functional and Molecular Effects of Mercury Compounds on the Human OCTN1 Cation Transporter: C50 and C136 Are the Targets for Potent Inhibition

(2014) Michele Galluccio et al.   TOXICOLOGICAL SCIENCES

Prodrug-based nanoparticulate drug delivery strategies for cancer therapy

(2014) Cong Luo et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Pharmacological doses of niacin stimulate the expression of genes involved in carnitine uptake and biosynthesis and improve the carnitine status of obese Zucker rats

(2014) Aline Couturier et al.   BMC Pharmacology & Toxicology

Gut microbiota metabolism of l-carnitine and cardiovascular risk

(2013) John R. Ussher et al.   ATHEROSCLEROSIS

Genetically modified mouse models for oral drug absorption and disposition

(2013) Seng Chuan Tang et al.   CURRENT OPINION IN PHARMACOLOGY

Molecular Modeling and Ligand Docking for Solute Carrier (SLC) Transporters

(2013) Avner Schlessinger et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Functional Expression of Organic Cation/carnitine Transporter 2 (OCTN2/SLC22A5) in Human Brain Capillary Endothelial Cell Line hCMEC/D3, a Human Blood-brain Barrier Model

(2013) Takashi Okura et al.   Drug Metabolism and Pharmacokinetics

l-carnitine supplementation as a potential antioxidant therapy for inherited neurometabolic disorders

(2013) Graziela S. Ribas et al.   GENE

Involvement of Carnitine/Organic Cation Transporter OCTN1/SLC22A4 in Gastrointestinal Absorption of Metformin

(2013) Noritaka Nakamichi et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

The SLC22 family with transporters of organic cations, anions and zwitterions

(2013) Hermann Koepsell   MOLECULAR ASPECTS OF MEDICINE

Functional Analysis of Novel Variants in the Organic Cation/Ergothioneine Transporter 1 Identified in Singapore Populations

(2013) Dorothy Su Lin Toh et al.   MOLECULAR PHARMACEUTICS

Crystal structure of a eukaryotic phosphate transporter

(2013) Bjørn P. Pedersen et al.   NATURE

Intestinal microbiota metabolism of l-carnitine, a nutrient in red meat, promotes atherosclerosis

(2013) Robert A Koeth et al.   NATURE MEDICINE

Caveolin-1 - A Novel Interacting Partner of Organic Cation/Carnitine Transporter (Octn2): Effect of Protein Kinase C on This Interaction in Rat Astrocytes

(2013) Magdalena Czeredys et al.   PLoS One

Molecular Mechanism of Inhibition of the Mitochondrial Carnitine/Acylcarnitine Transporter by Omeprazole Revealed by Proteoliposome Assay, Mutagenesis and Bioinformatics

(2013) Annamaria Tonazzi et al.   PLoS One

In-cell Western™ detection of organic cation transporters in bronchial epithelial cell layers cultured at an air–liquid interface on Transwell ® inserts

(2013) Manali Mukherjee et al.   JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS

Proteoliposomes as Tool for Assaying Membrane Transporter Functions and Interactions with Xenobiotics

(2013) Mariafrancesca Scalise et al.   Pharmaceutics

Over-expression in Escherichia coli, purification and reconstitution in liposomes of the third member of the OCTN sub-family: The mouse carnitine transporter OCTN3

(2012) Mariafrancesca Scalise et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Pharmacological and pathophysiological roles of carnitine/organic cation transporters (OCTNs: SLC22A4, SLC22A5 and Slc22a21)

(2012) Ikumi Tamai   BIOPHARMACEUTICS & DRUG DISPOSITION

SLC22A5/OCTN2 expression in breast cancer is induced by estrogen via a novel intronic estrogen-response element (ERE)

(2012) Chunyu Wang et al.   BREAST CANCER RESEARCH AND TREATMENT

Three-Dimensional Structures of Membrane Proteins from Genomic Sequencing

(2012) Thomas A. Hopf et al.   CELL

Human OCTN2 (SLC22A5) is down-regulated in virus- and nonvirus-mediated cancer

(2012) Mariafrancesca Scalise et al.   CELL BIOCHEMISTRY AND FUNCTION

Acylcarnitines

(2012) Marieke G. Schooneman et al.   DIABETES

Regulation by physiological cations of acetylcholine transport mediated by human OCTN1 (SLC22A4). Implications in the non-neuronal cholinergic system

(2012) Lorena Pochini et al.   LIFE SCIENCES

Strategies of Bacterial Over Expression of Membrane Transporters Relevant in Human Health: The Successful Case of the Three Members of OCTN Subfamily

(2012) Cesare Indiveri et al.   MOLECULAR BIOTECHNOLOGY

Functional expression of carnitine/organic cation transporter OCTN1 in mouse brain neurons: Possible involvement in neuronal differentiation

(2012) Noritaka Nakamichi et al.   NEUROCHEMISTRY INTERNATIONAL

Polymorphisms in OCTN1 and OCTN2 transporters genes are associated with prolonged time to progression in unresectable gastrointestinal stromal tumours treated with imatinib therapy

(2012) Sabrina Angelini et al.   PHARMACOLOGICAL RESEARCH

Inhibition of the OCTN2 carnitine transporter by HgCl2and methylmercury in the proteoliposome experimental model: insights in the mechanism of toxicity

(2012) Lorena Pochini et al.   TOXICOLOGY MECHANISMS AND METHODS

Vegetarians have a reduced skeletal muscle carnitine transport capacity

(2011) F. B. Stephens et al.   AMERICAN JOURNAL OF CLINICAL NUTRITION

The human OCTN1 (SLC22A4) reconstituted in liposomes catalyzes acetylcholine transport which is defective in the mutant L503F associated to the Crohn's disease

(2011) Lorena Pochini et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Expression of muscarinic receptors by human macrophages

(2011) A. Koarai et al.   EUROPEAN RESPIRATORY JOURNAL

Association between OCTN1/2 gene polymorphisms (1672C-T, 207G-C) and susceptibility of Crohn's disease: a meta-analysis

(2011) Chao Xuan et al.   INTERNATIONAL JOURNAL OF COLORECTAL DISEASE

Expression and functional analysis of intestinal organic cation/l-carnitine transporter (OCTN) in Crohn's Disease

(2011) Marc Girardin et al.   Journal of Crohns & Colitis

Synthesis and in vitro characterization of drug conjugates of l-carnitine as potential prodrugs that target human Octn2

(2011) Lei Diao et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Over-Expression in E. coli and Purification of the Human OCTN2 Transport Protein

(2011) Michele Galluccio et al.   MOLECULAR BIOTECHNOLOGY

Metabolic Agents that Enhance ATP can Improve Cognitive Functioning: A Review of the Evidence for Glucose, Oxygen, Pyruvate, Creatine, and l-Carnitine

(2011) Lauren Owen et al.   Nutrients

Upregulation of mammary gland OCTNs maintains carnitine homeostasis in suckling infants

(2010) Anne-Marie Lamhonwah et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Functional Expression of Carnitine/Organic Cation Transporter OCTN1/SLC22A4 in Mouse Small Intestine and Liver

(2010) T. Sugiura et al.   DRUG METABOLISM AND DISPOSITION

Metabolism of acetyl-l-carnitine for energy and neurotransmitter synthesis in the immature rat brain

(2010) Susanna Scafidi et al.   JOURNAL OF NEUROCHEMISTRY

Membrane transporters in drug development

(2010)   NATURE REVIEWS DRUG DISCOVERY

High Affinity Carnitine Transporters from OCTN Family in Neural Cells

(2010) Elżbieta Januszewicz et al.   NEUROCHEMICAL RESEARCH

A Large-Scale, Consortium-Based Genomewide Association Study of Asthma

(2010) Miriam F. Moffatt et al.   NEW ENGLAND JOURNAL OF MEDICINE

Role of carnitine in disease

(2010) Judith L Flanagan et al.   Nutrition & Metabolism

Gene Knockout and Metabolome Analysis of Carnitine/Organic Cation Transporter OCTN1

(2010) Yukio Kato et al.   PHARMACEUTICAL RESEARCH

Low availability of carnitine precursors as a possible reason for the diminished plasma carnitine concentrations in pregnant women

(2010) Robert Ringseis et al.   BMC Pregnancy and Childbirth

Hepatic uptake of γ-butyrobetaine, a precursor of carnitine biosynthesis, in rats

(2009) Masaharu Fujita et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

Carnitine/Organic Cation Transporter OCTN2 (Slc22a5) Is Responsible for Renal Secretion of Cephaloridine in Mice

(2009) T. Kano et al.   DRUG METABOLISM AND DISPOSITION

Toward a Systems Level Understanding of Organic Anion and Other Multispecific Drug Transporters: A Remote Sensing and Signaling Hypothesis

(2009) S.-Y. Ahn et al.   MOLECULAR PHARMACOLOGY

Carnitine Conjugate of Nipecotic Acid: A New Example of Dual Prodrug

(2009) Carmela Napolitano et al.   MOLECULES

Structure of a prokaryotic virtual proton pump at 3.2 Å resolution

(2009) Yiling Fang et al.   NATURE

Inactivation by omeprazole of the carnitine transporter (OCTN2) reconstituted in liposomes

(2008) Lorena Pochini et al.   CHEMICO-BIOLOGICAL INTERACTIONS

Involvement of the Pyrilamine Transporter, a Putative Organic Cation Transporter, in Blood-Brain Barrier Transport of Oxycodone

(2008) T. Okura et al.   DRUG METABOLISM AND DISPOSITION

Carnitine in metabolic disease: Potential for pharmacological intervention

(2008) A ARDUINI et al.   PHARMACOLOGY & THERAPEUTICS

Contributions of phosphorylation to regulation of OCTN2 uptake of carnitine are minimal in BeWo cells

(2007) Erik Rytting et al.   BIOCHEMICAL PHARMACOLOGY

Synthesis and characterization of carnitine nitro-derivatives

(2007) Oriana Piermatti et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Expression patterns of the organic cation/carnitine transporter family in adult murine brain

(2007) Anne Marie Lamhonwah et al.   BRAIN & DEVELOPMENT