Relationships between Inhibition, Transport and Enhanced Transport via the Organic Cation Transporter 1

Cellular Uptake of Psychostimulants – Are High- and Low-Affinity Organic Cation Transporters Drug Traffickers?

(2021) Ole Jensen et al.   Frontiers in Pharmacology

Identification of Novel High-Affinity Substrates of OCT1 Using Machine Learning-Guided Virtual Screening and Experimental Validation

(2021) Ole Jensen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Update on drug-drug interaction at organic cation transporters: mechanisms, clinical impact, and proposal for advanced in vitro testing

(2021) Hermann Koepsell   Expert Opinion on Drug Metabolism & Toxicology

Highly accurate protein structure prediction with AlphaFold

(2021) John Jumper et al.   NATURE

Overlap and Specificity in the Substrate Spectra of Human Monoamine Transporters and Organic Cation Transporters 1, 2, and 3

(2021) Lukas Gebauer et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Molecular basis for stereoselective transport of fenoterol by the organic cation transporters 1 and 2

(2021) Lukas Gebauer et al.   BIOCHEMICAL PHARMACOLOGY

Differences in metformin and thiamine uptake between human and mouse organic cation transporter OCT1: structural determinants and potential consequences for intrahepatic concentrations

(2020) Marleen J. Meyer et al.   DRUG METABOLISM AND DISPOSITION

Structural identification of a hotspot on CFTR for potentiation

(2019) Fangyu Liu et al.   SCIENCE

Pharmacokinetic Drug‐Drug Interactions Between Trospium Chloride and Ranitidine Substrates of Organic Cation Transporters in Healthy Human Subjects

(2019) Bayew Tsega Abebe et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Variability and Heritability of Thiamine Pharmacokinetics With Focus on OCT1 Effects on Membrane Transport and Pharmacokinetics in Humans

(2019) Ole Jensen et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Pharmacokinetics of Organic Cation Transporter 1 (OCT1) Substrates in Oct1/2 Knockout Mice and Species Difference in Hepatic OCT1-mediated Uptake

(2019) Bridget L. Morse et al.   DRUG METABOLISM AND DISPOSITION

Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1

(2019) Marleen J. Meyer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Stereoselective cell uptake of adrenergic agonists and antagonists by organic cation transporters

(2019) Ole Jensen et al.   BIOCHEMICAL PHARMACOLOGY

Organic Cation Transporters in Health and Disease

(2019) Hermann Koepsell   PHARMACOLOGICAL REVIEWS

Assessment of Substrate Dependent Ligand Interactions at the Organic Cation Transporter OCT2 Using Six Model Substrates

(2018) Philip J Sandoval et al.   MOLECULAR PHARMACOLOGY

Organic cation transporter 1 (OCT1) modulates multiple cardiometabolic traits through effects on hepatic thiamine content

(2018) Xiaomin Liang et al.   PLOS BIOLOGY

Multiple binding sites in organic cation transporters require sophisticated procedures to identify interactions of novel drugs

(2018) Hermann Koepsell   BIOLOGICAL CHEMISTRY

Rat Organic Cation Transporter 1 Contains Three Binding Sites for Substrate 1-Methyl-4-phenylpyridinium per Monomer

(2018) Thorsten Keller et al.   MOLECULAR PHARMACOLOGY

Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1)

(2017) Eugene C. Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Effects of genetic polymorphisms on the OCT1 and OCT2-mediated uptake of ranitidine

(2017) Marleen Julia Meyer et al.   PLoS One

Primary Carnitine Deficiency and Newborn Screening for Disorders of the Carnitine Cycle

(2016) Nicola Longo   ANNALS OF NUTRITION AND METABOLISM

OCT1 mediates hepatic uptake of sumatriptan and loss-of-functionOCT1polymorphisms affect sumatriptan pharmacokinetics

(2016) J Matthaei et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

X-ray structures and mechanism of the human serotonin transporter

(2016) Jonathan A. Coleman et al.   NATURE

Substrate-Dependent Inhibition of the Human Organic Cation Transporter OCT2: A Comparison of Metformin with Experimental Substrates

(2015) Kristina Hacker et al.   PLoS One

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

Verapamil decreases the glucose-lowering effect of metformin in healthy volunteers

(2014) Sung Kweon Cho et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Mechanistic interpretation of conventional Michaelis–Menten parameters in a transporter system

(2014) Diana Vivian et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

ABCC3 and OCT1 genotypes influence pharmacokinetics of morphine in children

(2014) Raja Venkatasubramanian et al.   PHARMACOGENOMICS

Identification of Novel Substrates and Structure–Activity Relationship of Cellular Uptake Mediated by Human Organic Cation Transporters 1 and 2

(2013) Ramon Hendrickx et al.   JOURNAL OF MEDICINAL CHEMISTRY

Computational Modeling to Accelerate the Identification of Substrates and Inhibitors for Transporters That Affect Drug Disposition

(2012) S Ekins et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Human metabolic individuality in biomedical and pharmaceutical research

(2011) Karsten Suhre et al.   NATURE

Inhibitory and facilitory actions of isocyanine derivatives at human and rat organic cation transporters 1, 2 and 3: A comparison to human α1- and α2-adrenoceptor subtypes

(2010) Anne Amphoux et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Expression of organic cation transporters OCT1 (SLC22A1) and OCT3 (SLC22A3) is affected by genetic factors and cholestasis in human liver

(2009) Anne T. Nies et al.   HEPATOLOGY

AutoDock Vina: Improving the speed and accuracy of docking with a new scoring function, efficient optimization, and multithreading

(2009) Oleg Trott et al.   JOURNAL OF COMPUTATIONAL CHEMISTRY

Transport of Lamivudine [(-)- -L-2',3'-Dideoxy-3'-thiacytidine] and High-Affinity Interaction of Nucleoside Reverse Transcriptase Inhibitors with Human Organic Cation Transporters 1, 2, and 3

(2009) G. Minuesa et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Five Amino Acids in the Innermost Cavity of the Substrate Binding Cleft of Organic Cation Transporter 1 Interact with Extracellular and Intracellular Corticosterone

(2009) C. Volk et al.   MOLECULAR PHARMACOLOGY

Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770

(2009) F. Van Goor et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural Requirements for Drug Inhibition of the Liver Specific Human Organic Cation Transport Protein 1

(2008) Gustav Ahlin et al.   JOURNAL OF MEDICINAL CHEMISTRY