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Expression of Selected Pharmacologically Relevant Transporters in Murine Non-Parenchymal Liver Cells Compared to Hepatocytes Open
Primary hepatocytes are widely used in preclinical drug development, with their transporter expression being well-characterized. However, less is known about non-parenchymal liver cells (NPCs), which constitute 40% of the liver’s cell popu…
Ex vivo perfusion model of mouse liver and its application to analyze the effects of OCT1 deficiency Open
Introduction The liver plays a critical role in drug pharmacokinetics. In in vivo experiments, it is difficult to isolate the liver’s contribution to drug systemic concentrations from that of the intestine and kidneys. Rat liver perfusion …
Increased coproporphyrin serum levels in healthy volunteers treated with the cholesterol uptake inhibitor ezetimibe Open
Ezetimibe undergoes glucuronidation that results in the active metabolite ezetimibe phenoxy‐glucuronide (ezetimibe‐glucuronide). This phase‐II metabolite was shown to interact with the clinically relevant hepatic transporter organic anion …
Various effects of repeated rifampin dosing on coproporphyrin levels in humans Open
In recent years, the identification of endogenous substrates as biomarkers became an uprising topic. Particularly coproporphyrins (CPs), byproducts of heme biosynthesis, are intensely investigated as biomarkers for predicting interactions …
The influence of OATP2B1 and atorvastatin on coproporphyrin isomers in rats Open
Coproporphyrin I (CPI) and III (CPIII) are discussed as biomarkers for organic anion transporting polypeptides (OATPs). We report on CPI and CPIII levels in wildtype, rSlco2b1-knockout, and SLCO2B1-humanized rats at baseline and after admi…
View article: The Putative S1PR1 Modulator ACT-209905 Impairs Growth and Migration of Glioblastoma Cells In Vitro
The Putative S1PR1 Modulator ACT-209905 Impairs Growth and Migration of Glioblastoma Cells In Vitro Open
Glioblastoma (GBM) is still a deadly tumor due to its highly infiltrative growth behavior and its resistance to therapy. Evidence is accumulating that sphingosine-1-phosphate (S1P) acts as an important tumor-promoting molecule that is invo…
View article: Data from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme
Data from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme Open
Purpose:Apoptotic dysregulation, redox adaptive mechanisms, and resilience to hypoxia are major causes of glioblastoma (GBM) resistance to therapy. Commonly known as crucial factors in energy metabolism, OCTN2 (SLC22A5) and its substrate L…
View article: Supplementary Figure S1 from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme
Supplementary Figure S1 from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme Open
Survival analysis of patients with primary GBM dependent on therapy and resection status
View article: Data from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme
Data from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme Open
Purpose:Apoptotic dysregulation, redox adaptive mechanisms, and resilience to hypoxia are major causes of glioblastoma (GBM) resistance to therapy. Commonly known as crucial factors in energy metabolism, OCTN2 (SLC22A5) and its substrate L…
View article: Supplementary Figure S2 from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme
Supplementary Figure S2 from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme Open
Expression and survival analyses of CPT1A and CPT1C in GBM specimens
View article: Supplementary Text from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme
Supplementary Text from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme Open
Additional information on the immunoblot analysis, cell line characteristics and our glioma mouse model
View article: Supplementary Text from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme
Supplementary Text from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme Open
Additional information on the immunoblot analysis, cell line characteristics and our glioma mouse model
View article: Supplementary Figure S2 from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme
Supplementary Figure S2 from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme Open
Expression and survival analyses of CPT1A and CPT1C in GBM specimens
View article: Supplementary Figure S1 from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme
Supplementary Figure S1 from <i>L</i>-Carnitine–Mediated Tumor Cell Protection and Poor Patient Survival Associated with OCTN2 Overexpression in Glioblastoma Multiforme Open
Survival analysis of patients with primary GBM dependent on therapy and resection status
PIM1 Inhibition Affects Glioblastoma Stem Cell Behavior and Kills Glioblastoma Stem-like Cells Open
Despite comprehensive therapy and extensive research, glioblastoma (GBM) still represents the most aggressive brain tumor in adults. Glioma stem cells (GSCs) are thought to play a major role in tumor progression and resistance of GBM cells…
Differences in transport function of the human and rat orthologue of the Organic Anion Transporting Polypeptide 2B1 (OATP2B1) Open
The human drug transporter Organic Anion Transporting Polypeptide (hOATP)2B1 facilitates cellular uptake of its substrates. Various studies suggest that hOATP2B1 is involved in intestinal absorption, but preclinical evaluations performed i…
Correction to: Tooth loss and adiposity: possible role of carnitine transporter (OCTN1/2) polymorphisms in women but not in men Open
The online version of the original article can be found at https://doi.org/10.1007/s00784-020–03594-w
Expression and Function of Organic Anion Transporting Polypeptides in the Human Brain: Physiological and Pharmacological Implications Open
The central nervous system (CNS) is an important pharmacological target, but it is very effectively protected by the blood–brain barrier (BBB), thereby impairing the efficacy of many potential active compounds as they are unable to cross t…
Chiral Pharmacokinetics and Metabolite Profile of Prolonged-release Ketamine Tablets in Healthy Human Subjects Open
Background The anesthetic ketamine after intravenous dosing is nearly completely metabolized to R- and S-stereoisomers of the active norketamine (analgesic, psychoactive) and 2,6-hydroxynorketamine (potential analgesic, antidepressant) as …
OATP2B1 – The underrated member of the organic anion transporting polypeptide family of drug transporters? Open
The organic anion transporting polypeptide 2B1 (OATP2B1) was one of the first cloned members of the SLCO family. However, its physiological and pharmacological role is still poorly understood, and object of a current debate on the transpor…
Tooth loss and adiposity: possible role of carnitine transporter (OCTN1/2) polymorphisms in women but not in men Open
Objective SLC22A4/5 single nucleotide polymorphisms (SNPs) have been reported to affect inflammatory diseases. We report the relationship of these polymorphisms with adiposity and tooth loss as elucidated in a 10-year follow-up study. Meth…
Neurosteroid Transport in the Brain: Role of ABC and SLC Transporters Open
Neurosteroids, comprising pregnane, androstane, and sulfated steroids can alter neuronal excitability through interaction with ligand-gated ion channels and other receptors and have therefore a therapeutic potential in several brain disord…