Polyglutamation of methotrexate. Is methotrexate a prodrug?
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چکیده
منابع مشابه
TSPO Ligand-Methotrexate Prodrug Conjugates: Design, Synthesis, and Biological Evaluation
The 18-kDa translocator protein (TSPO) is a potential mitochondrial target for drug delivery to tumors overexpressing TSPO, including brain cancers, and selective TSPO ligands have been successfully used to selectively deliver drugs into the target. Methotrexate (MTX) is an anticancer drug of choice for the treatment of several cancers, but its permeability through the blood brain barrier (BBB)...
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Influx of [3H]methotrexate into freshly isolated hepatocytes in suspension is mediated by two routes, one with a high affinity (Km = 5.9 microM) and another with a low affinity for methotrexate. Both transport routes are equally sensitive to the sulfhydryl group inhibitor, p-chloromercuriphenylsulfonic acid, alterations in temperature, substitution of extracellular Na+ with choline, and inhibit...
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BACKGROUND The JAK/STAT pathway transduces signals from multiple cytokines and controls haematopoiesis, immunity and inflammation. In addition, pathological activation is seen in multiple malignancies including the myeloproliferative neoplasms (MPNs). Given this, drug development efforts have targeted the pathway with JAK inhibitors such as ruxolitinib. Although effective, high costs and side e...
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Methotrexate is an antineopalstic agent widely used in low dose to treat patients with rheumatoid arthritis. It is known to induce micronuclei at multiple doses in rats. The present study investigates the effect of vitamin A on methotrexate-induced micronuclei in rat bone marrow erythrocytes. Male wistar rats were (n=5) injected with 0, 8, 16 and20mg/kg methotrexate (single i.p dose). A group o...
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Although Methotrexate (MTX) is an effective drug for the treatment of acute lymphoblastic leukemia (ALL), the toxicity remains a significant problem. In this prospective study, fifty-four patients with ALL were enrolled. 3 g or 5 g MTX/m(2) was administered over 24 hours. Serum MTX concentrations were determined in 24, 48, and 96 hours after MTX infusion. Serum creatinine concentrations and cre...
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ژورنال
عنوان ژورنال: Journal of Clinical Investigation
سال: 1985
ISSN: 0021-9738
DOI: 10.1172/jci112088