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Cisplatin nephrotoxicity is critically mediated via the human organic cation transporter 2.
Cis-platin is an effective anti-neoplastic agent, but it is also highly nephrotoxic. Here, we clearly identify the human organic cation transporter 2 (hOCT2) as the critical transporter forExpand
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Long‐term activation of SAPK/JNK, p38 kinase and fas‐L expression by cisplatin is attenuated in human carcinoma cells that acquired drug resistance
Tumor cells chronically exposed to cisplatin (cDDP) acquire cDDP resistance that impacts tumor therapy. To elucidate the mechanism of acquired cDDP resistance (ACR), we compared HeLa cells thatExpand
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Relevance of drug uptake and efflux for cisplatin sensitivity of tumor cells.
Platinum sensitivity and platinum resistance may involve altered activity of transport proteins. In order to assess the role of drug uptake and efflux in this phenomenon, we compared the expressionExpand
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The Raf kinase inhibitor BAY 43-9006 reduces cellular uptake of platinum compounds and cytotoxicity in human colorectal carcinoma cell lines
Raf kinase plays a central role in oncogenic signaling and acts as a downstream effector of Ras in the extracellular signal-regulated (ERK) kinase pathway. BAY 43-9006 (BAY) is a novel signalExpand
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Pharmacokinetic/Pharmacodynamic Modelling of Receptor Internalization with CRTH2 Antagonists to Optimize Dose Selection
Background and ObjectiveThe chemoattractant receptor-homologous molecule expressed on T helper-2 cells (CRTH2) is a G-protein-coupled receptor for prostaglandin D2 (PGD2), a key mediator inExpand
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Assessment of platinum sensitivity in human tumor cells.
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Development of a decision-making biomarker for CRTH2 antagonism in clinical studies
Abstract Biomarkers have shown to improve success rates in the development of novel drugs, providing essential information in the early phases of clinical development for decision-making.Expand
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It was shown that parasympathomimetic drugs can increase the pain threshold, produce antiallodynic and antihyperalgesic effects in neuropathic pain. However, their peripheral side effects andExpand
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Modeling the Two -Peak Phenomenon in Pharmacokinetics Using a Gut Passage Model with two Absorption Sites
Background  The first study with a new compound in humans showed PK characteristics that can be characterized by a single compartment model.  Higher doses exhibited a two-peak phenomenon: a secondExpand