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Download Deoxynucleoside Analogs In Cancer Therapy by Marçal Pastor-Anglada MSc, PhD (auth.), Godefridus J. Peters PDF

By Marçal Pastor-Anglada MSc, PhD (auth.), Godefridus J. Peters PhD (eds.)

Emerging as a massive new quantity within the popular melanoma Drug Discovery and improvement™ sequence, Deoxynucleoside Analogs in melanoma treatment expertly summarizes the present prestige of improvement and alertness of deoxynucleoside analogs. Authoritative up to date experiences are awarded through scientists popular of their particular components and all contributions comprise beneficial sound suggestion on constitution and topics.
geared up into numerous sections, the 1st half covers basic points of drug uptake and metabolism and explains how novel expertise has enabled a quick enlargement of this box. the second one half is anxious with a few particular medications together with cytarabine, gemcitabine, troxacitabine, clofarabine and Ara-G. the ultimate part covers pharmacokinetics, prodrugs, and particular purposes corresponding to radiosensitization, gene remedy, and using deoxynucleoside analogs as tracers.
all through Deoxynucleoside Analogs in melanoma remedy, the point of interest is on novel facets of deoxynucleoside analogs within the medical context, in addition to on unforeseen pursuits of those compounds, reminiscent of their particular task opposed to mobilephone cycle-dependent kinases or oncogenes. The wealth of data awarded right here can be utilized to layout rational mixtures geared toward inhibiting numerous mobile signaling pathways, or combining inhibition of assorted ambitions. Deoxynucleoside Analogs in melanoma remedy has been designed particularly to facilitate such an interplay among a variety of fields.

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31. Osato DH, Huang CC, Kawamoto M, et al. Functional characterization in yeast of genetic variants in the equilibrative nucleoside transporter, ENT1. Pharmacogenetics 2003;13:297–301. 32. Gray JH, Mangravite LM, Owen RP, et al. Functional and genetic diversity in the concentrative nucleoside transporter, CNT1, in human populations. Mol Pharmacol 2004;65:512–519. 33. Lai Y, Lee EW, Ton CC, Vijay S, Zhang H, Unadkat JD. Conserved residues F316 and G476 in the concentrative nucleoside transporter 1 (hCNT1) impact guanosine sensitivity and membrane expression, respectively.

13. Chandrasena G, Giltay R, Patil SD, Bakken A, Unadkat JD. Functional expression of human intestinal Na+-dependent and Na+-independent nucleoside transporters in Xenopus laevis oocytes. Biochem Pharmacol 1997;53: 1909–1918. 24 Pastor-Anglada and Casado 14. Ritzel MW, Yao SY, Ng AM, Mackey JR, Cass CE, Young JD. Molecular cloning, functional expression and chromosomal localization of a cDNA encoding a human Na+/nucleoside cotransporter (hCNT2) selective for purine nucleosides and uridine. Mol Membr Biol 1998;15:203–211.

CdA is an excellent substrate for dCK in vitro (34) as well as in vivo, and its main product, Cl-dAMP, accumulates in human lymphocytes during short-term incubations, during which the activity of dCK increased two to four times (35). The 38 Staub and Eriksson same enhancement of dCK activity occurred on preincubation with a variety of nonnucleoside genotoxic agents such as aphidicolin (35), etoposide (VP16) (36,37), taxol, and even the G protein modulator sodium fluoride (38,39). γ-Irradiation (40) and UV-C irradiation (41) also augmented dCK activity in different lymphoid cells.

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