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Wernig, Gerlinde; Kharas, Michael G.; Okabe, Rachel; Moore, Sandra A.; Leeman, Dena S.; Cullen, Dana E.; Gozo, Maricel; McDowell, Elizabeth P.; Levine, Ross L.; Doukas, John; Mak, Chi Ching; Noronha, Glenn; Martin, Michael; Ko, Yon D.; Lee, Benjamin H.; Soll, Richard M.; Tefferi, Ayalew; Hood, John D.; Gilliland, D. Gary
Cancer cell, 04/2008, Letnik: 13, Številka: 4Journal Article
We report that TG101348, a selective small-molecule inhibitor of JAK2 with an in vitro IC50 of ∼3 nM, shows therapeutic efficacy in a murine model of myeloproliferative disease induced by the JAK2V617F mutation. In treated animals, there was a statistically significant reduction in hematocrit and leukocyte count, a dose-dependent reduction/elimination of extramedullary hematopoiesis, and, at least in some instances, evidence for attenuation of myelofibrosis. There were no apparent toxicities and no effect on T cell number. In vivo responses were correlated with surrogate endpoints, including reduction/elimination of JAK2V617F disease burden assessed by quantitative genomic PCR, suppression of endogenous erythroid colony formation, and in vivo inhibition of JAK-STAT signal transduction as assessed by flow cytometric measurement of phosphorylated Stat5.
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Dostop do baze podatkov JCR je dovoljen samo uporabnikom iz Slovenije. Vaš trenutni IP-naslov ni na seznamu dovoljenih za dostop, zato je potrebna avtentikacija z ustreznim računom AAI.
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Vir: Osebne bibliografije
in: SICRIS
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