Search Results - "ERKER, Thomas"
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A novel prodrug-based strategy to increase effects of bumetanide in epilepsy
Published in Annals of neurology (01-04-2014)“…Objective There is considerable interest in using bumetanide, a chloride importer Na‐K‐Cl cotransporter antagonist, for treatment of neurological diseases,…”
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Tariquidar and elacridar are dose-dependently transported by P-glycoprotein and Bcrp at the blood-brain barrier: a small-animal positron emission tomography and in vitro study
Published in Drug metabolism and disposition (01-04-2013)“…Elacridar (ELC) and tariquidar (TQD) are generally thought to be nontransported inhibitors of P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP),…”
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3
PET and SPECT radiotracers to assess function and expression of ABC transporters in vivo
Published in Current drug metabolism (01-10-2011)“…Adenosine triphosphate-binding cassette (ABC) transporters, such as P-glycoprotein (Pgp, ABCB1), breast cancer resistance protein (BCRP, ABCG2) and multidrug…”
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Resveratrol post-transcriptionally regulates pro-inflammatory gene expression via regulation of KSRP RNA binding activity
Published in Nucleic acids research (10-11-2014)“…Resveratrol shows beneficial effects in inflammation-based diseases like cancer, cardiovascular and chronic inflammatory diseases. Therefore, the molecular…”
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Role of NKCC1 Activity in Glioma K+ Homeostasis and Cell Growth: New Insights With the Bumetanide-Derivative STS66
Published in Frontiers in physiology (31-07-2020)“…Introduction: Na + -K + -2Cl − cotransporter isoform 1 (NKCC1) is important in regulating intracellular K + and Cl − homeostasis and cell volume. In this…”
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6
GABAA receptor modulation by piperine and a non-TRPV1 activating derivative
Published in Biochemical pharmacology (15-06-2013)“…The action of piperine (the pungent component of pepper) and its derivative SCT-66 ((2E,4E)-5-(1,3-benzodioxol-5-yl))-N,N-diisobutyl-2,4-pentadienamide) on…”
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Novel Promising Estrogenic Receptor Modulators: Cytotoxic and Estrogenic Activity of Benzanilides and Dithiobenzanilides
Published in PloS one (2016)“…The cytotoxicity of 27 benzanilides and dithiobenzanilides built on a stilbene scaffold and possessing various functional groups in aromatic rings previously…”
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Synthesis and in vivo evaluation of [11C]tariquidar, a positron emission tomography radiotracer based on a third-generation P-glycoprotein inhibitor
Published in Bioorganic & medicinal chemistry (01-08-2010)“…The aim of this study was to develop a positron emission tomography (PET) tracer based on the dual P-glycoprotein (P-gp) breast cancer resistance protein…”
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Synthesis and Small-Animal Positron Emission Tomography Evaluation of [11C]-Elacridar As a Radiotracer to Assess the Distribution of P-Glycoprotein at the Blood−Brain Barrier
Published in Journal of medicinal chemistry (08-10-2009)“…With the aim to develop a positron emission tomography (PET) tracer to assess the distribution of P-glycoprotein (P-gp) at the blood−brain barrier (BBB) in…”
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10
Foam cell specific LXRα ligand
Published in PloS one (25-02-2013)“…The liver X receptor α (LXRα) is a ligand-dependent nuclear receptor and the major regulator of reverse cholesterol transport in macrophages. This makes it an…”
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Resveratrol blocks Akt activation in angiotensin II-or EGF-stimulated vascular smooth muscle cells in a redox-independent manner
Published in Cardiovascular research (01-04-2011)“…Resveratrol (RV), an antioxidant, inhibits angiotensin II (Ang II)-induced hypertrophy and Ang II- or epidermal growth factor (EGF)-induced Akt phosphorylation…”
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Synthesis of Novel Curcumin Analogues and Their Evaluation as Selective Cyclooxygenase-1 (COX-1) Inhibitors
Published in Chemical & pharmaceutical bulletin (2007)“…Curcumin, a major yellow pigment and active component of turmeric, has been shown to possess anti-inflammatory and anti-cancer activities. Recent studies have…”
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Antioxidant activity of resveratrol, piceatannol and 3,3',4,4',5,5'-hexahydroxy-trans-stilbene in three leukemia cell lines
Published in Oncology reports (01-09-2006)“…trans-Resveratrol (t-RES) is one of the most relevant and extensively investigated stilbenes with a broad spectrum of biological activities. In contrast to the…”
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14
Using structural and mechanistic information to design novel inhibitors/substrates of P-glycoprotein
Published in Current topics in medicinal chemistry (01-12-2010)“…Design of inhibitors of P-glycoprotein still represents a challenging task for medicinal chemists. The polyspecificity of the transporter combined with the…”
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Novel Resveratrol Derivatives Induce Apoptosis and Cause Cell Cycle Arrest in Prostate Cancer Cell Lines
Published in Anticancer research (01-09-2007)“…Background: Resveratrol (RV), a naturally occurring phytoalexin, exerts manifold biological effects against a variety of human tumor cell lines. In this study,…”
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16
Impaired chloride homeostasis in epilepsy: Molecular basis, impact on treatment, and current treatment approaches
Published in Pharmacology & therapeutics (Oxford) (01-01-2020)“…Epilepsies represent one of the most common neurological diseases worldwide. They are characterized by recurrent spontaneous seizures with severe impact on a…”
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Functional characterization of novel bumetanide derivatives for epilepsy treatment
Published in Neuropharmacology (01-01-2020)“…Temporal lobe epilepsy (TLE) is the most common type of focal epilepsies, affecting approximately 35 million people worldwide. Despite the introduction of…”
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Synthesis of 1,2-Disubstituted Imidazoles via Cross-Coupling and Substitution Reactions
Published in Heterocycles (01-11-2005)Get full text
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Effects of Novel Synthesized Pyridothiazines on Various Guinea Pig Heart Muscle Preparations
Published in Biological & Pharmaceutical Bulletin (01-09-2004)“…Calcium channel blockers have become important tools in the treatment of cardiovascular disorders and other diseases. Hybridization of well established calcium…”
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Multiple blood-brain barrier transport mechanisms limit bumetanide accumulation, and therapeutic potential, in the mammalian brain
Published in Neuropharmacology (01-05-2017)“…There is accumulating evidence that bumetanide, which has been used over decades as a potent loop diuretic, also exerts effects on brain disorders, including…”
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