Structure-Guided Identification of Phytochemical OCT2 Inhibitors and Their Functional Relevance to Cisplatin-Induced Cytotoxicity [PDF]
PharmaceuticsBackground: Organic cation transporter 2 (OCT2) mediates the renal uptake of cisplatin and is a principal contributor to its dose-limiting nephrotoxicity. Despite reports of OCT2 inhibition by various phytochemicals, the structure–activity relationships (
Hyerim Song +4 more
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Cell Reports, 2021 Summary: The transcription factors (TFs) that regulate inducible genes in activated neutrophils are not yet completely characterized. Herein, we show that the genomic distribution of the histone modification H3K27Ac, as well as PU.1 and C/EBPβ, two ...
Nicola Tamassia +2 more
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Acta Pharmaceutica Sinica B, 2019 Renal cell carcinoma (RCC) is one of the most common malignant tumors affecting the urogenital system, accounting for 90% of renal malignancies. Traditional chemotherapy options are often the front-line choice of regimen in the treatment of patients with
Zhiyuan Qin, Sheng Ye, Kui Zeng
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Gabapentin CNS exposure and analgesic response are modulated by OCT2 genotype in patients with chronic neuropathic pain [PDF]
Frontiers in PharmacologyIntroductionGabapentin (GBP) is commonly used for chronic neuropathic pain, yet its therapeutic response varies widely across individuals. As a substrate of the organic cation transporter 2 (OCT2), encoded by the SLC22A2 gene, GBP’s penetration into the ...
Lina Zhou +7 more
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Transport of the uremic toxin symmetric dimethylarginine (SDMA) by renal transport proteins [PDF]
Amino AcidsThe L-arginine derivative and uremic toxin symmetric dimethylarginine (SDMA) is an independent risk marker for total mortality and cardiovascular events.
Lorenz A. Scherpinski +3 more
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Influence of OCT2 gene variants on metformin efficacy in type 2 diabetes: insights into pharmacogenomics and drug interactions [PDF]
Journal of Translational MedicineMetformin, a widely prescribed treatment for type 2 diabetes mellitus (T2DM), demonstrates significant inter-individual variability in its therapeutic response. This variability is potentially driven by genetic differences in drug transporters.
Ma’mon M. Hatmal +9 more
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A strategy for evaluating the impact of processing of Chinese meteria medica on meridian tropism: the influence of salt-water processing of phellodendri chinensis cortex on renal transport proteins [PDF]
Frontiers in PharmacologyIntroductionThis study elucidated the potential mechanisms by which Phellodendri Chinensis Cortex with salt-water processing (SPC) enhances renal targeting efficacy, through investigating the effects of Phellodendri Chinensis Cortex (PC) on renal uptake ...
Yang Chen +8 more
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Bupropion decreases plasma levels of asymmetric dimethylarginine and ameliorates renal injury by modulation of Ddah1, Oatp4c1, Oct2, and Mate1 in rats with adenine-induced chronic renal injury [PDF]
Frontiers in PharmacologyObjectiveThe objective of the study was to investigate whether bupropion (BUP) or its circulation metabolites could decrease plasma level of asymmetric dimethylarginine (ADMA) and ameliorate renal injury by modulation of Ddah1, Oatp4c1, Oct2, and Mate1 ...
Lulu Huang +22 more
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Expression and Function of Organic Cation Transporter 2 in Pancreas
Frontiers in Cell and Developmental Biology, 2021 Organic cation transporters (OCT) play an important role in mediating cellular uptake of several pharmaceuticals, such as the antidiabetic drug metformin and the platinum-derived chemotherapeutics.
Sandra Schorn +6 more
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Frontiers in Medicine, 2022 Organic cation transporter 2 (OCT2), encoded by the SLC22A2 gene, is the main cation transporter on the basolateral membrane of proximal tubular cells. OCT2 facilitates the entry step of the vectorial transport of most cations from the peritubular space ...
Chao Han +11 more
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