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Exploring novel dilazep derivatives as hENT1 inhibitors and potentially covalent molecular tools.
Purinergic Signal
June 2024
Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, PO Box 9502, Leiden, The Netherlands.
The human equilibrative nucleoside transporter 1 (SLC29A1, hENT1) is a solute carrier that modulates the passive transport of nucleosides and nucleobases, such as adenosine. This nucleoside regulates various physiological processes, such as vasodilation and -constriction, neurotransmission and immune defense. Marketed drugs such as dilazep and dipyridamole have proven useful in cardiovascular afflictions, but the application of hENT1 inhibitors can be beneficial in a number of other diseases.
View Article and Find Full Text PDFResistance factors for the treatment of immunoglobulin A nephropathy with diffuse mesangial proliferation.
Nephrology (Carlton)
July 2014
Department of Pediatrics, Fukushima Medical University School of Medicine, Fukushima, Japan.
Aim: Some patients with severe immunoglobulin A nephropathy (IgAN) are resistant to multi-drug combination therapy; however, there have been few reports on the risk factors for non-responsiveness to treatment for severe IgAN. We, therefore, evaluated the risk factors for non-responsiveness to treatment in cases of severe IgAN.
Methods: We collected data on 44 children who had been diagnosed with IgAN with diffuse mesangial proliferation and treated with multi-drug combination therapy.
Predicting gemcitabine transport and toxicity in human pancreatic cancer cell lines with the positron emission tomography tracer 3'-deoxy-3'-fluorothymidine.
Biochem Pharmacol
February 2010
Department of Oncology, University of Alberta, Cross Cancer Institute, 11560 University Ave., Edmonton, Alberta, Canada.
The abundance of human equilibrative nucleoside transporter 1 (hENT1) has recently been shown to be a predictive marker of benefit from gemcitabine therapy in patients with pancreatic cancer. Since hENT1 is also important for the uptake of positron emission tomography (PET) tracer 3'-deoxy-3'-fluorothymidine (FLT) in various cultured human cell lines, this study was undertaken to determine if FLT uptake predicts gemcitabine uptake and/or toxicity in a panel of human pancreatic cancer cell lines (Capan-2, AsPC-1, BxPC-3, PL45, MIA PaCa-2, and PANC-1). Capan-2 cells displayed the lowest levels of (1) extracellular nitrobenzylmercaptopurine ribonucleoside (NBMPR) binding, which represents cell-surface hENT1, (2) FLT and gemcitabine uptake during short (1-45s) and prolonged (1h) periods, and (3) gemcitabine sensitivity.
View Article and Find Full Text PDFMutation of Trp29 of human equilibrative nucleoside transporter 1 alters affinity for coronary vasodilator drugs and nucleoside selectivity.
Biochem J
September 2008
Membrane Protein Research Group, University of Alberta, Edmonton, Alberta, Canada, T6G 2H7.
hENT1 (human equilibrative nucleoside transporter 1) is inhibited by nanomolar concentrations of various structurally distinct coronary vasodilator drugs, including dipyridamole, dilazep, draflazine, soluflazine and NBMPR (nitrobenzylmercaptopurine ribonucleoside). When a library of randomly mutated hENT1 cDNAs was screened using a yeast-based functional complementation assay for resistance to dilazep, a clone containing the W29G mutation was identified. Multiple sequence alignments revealed that this residue was highly conserved.
View Article and Find Full Text PDFA purine-selective nucleobase/nucleoside transporter in PK15NTD cells.
Am J Physiol Regul Integr Comp Physiol
June 2008
Department of Medicine, The Johns Hopkins University, Baltimore, MD 21205-2109, USA.
Nucleoside and nucleobase transporters are important for salvage of purines and pyrimidines and for transport of their analog drugs into cells. However, the pathways for nucleobase translocation in mammalian cells are not well characterized. We identified an Na-independent purine-selective nucleobase/nucleoside transport system in the nucleoside transporter-deficient PK15NTD cells.
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