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Dephosphorylation of WR-2721 with mouse tissue homogenates.

作者信息

Mori T, Nikaido O, Sugahara T

出版信息

Int J Radiat Oncol Biol Phys. 1984 Sep;10(9):1529-31. doi: 10.1016/0360-3016(84)90496-6.

DOI:10.1016/0360-3016(84)90496-6
PMID:6090356
Abstract

Mouse liver homogenate had an optimum pH of 8.6 to 8.8 for dephosphorylation of WR-2721 in the analyzed pH range from 5.2 to 10.0. At this optimum pH condition, the dephosphorylation activities of six mouse tissue homogenates were analyzed. Kidney, liver and small intestine homogenates showed higher dephosphorylation activities (935, 336 and 314 nmoles/mg protein/hr, respectively) than spleen and lung homogenates (86, 49 nmoles/mg protein/hr, respectively). Furthermore, serum did not show any dephosphorylation activity. The high activity found in liver homogenate agrees well with our previous data with mouse L cells. However, optimum pH from 8.6 to 8.8 in liver homogenate is quite different from the data reported by using Ehrlich ascites tumor cells (optimum pH was 5.6). Therefore, it is suggested that WR-2721 administered into mouse is efficiently dephosphorylated in certain tissues such as liver to its active form with the enzyme(s) different from that found in Ehrlich ascites tumor cells.

摘要

相似文献

1
Dephosphorylation of WR-2721 with mouse tissue homogenates.
Int J Radiat Oncol Biol Phys. 1984 Sep;10(9):1529-31. doi: 10.1016/0360-3016(84)90496-6.
2
WR-2721, its derivatives and their radioprotective effects on mammalian cells in culture.WR-2721及其衍生物以及它们对培养中的哺乳动物细胞的辐射防护作用。
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Distribution of 35S-labeled WR-2721 in normal and malignant tissues of the mouse1,2.35S标记的WR-2721在小鼠正常组织和恶性组织中的分布1,2 。
Radiat Res. 1976 Nov;68(2):284-91.
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In vitro metabolism of the phosphorothioate radioprotectors WR-2721 and WR-3689.
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Pharmacokinetics of WR-1065 in mouse tissue following treatment with WR-2721.
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[Distribution and elimination of aminoproplaminoethylthiophosphoric acid in dogs].[氨基丙氨基乙基硫代磷酸在犬体内的分布与消除]
Med Radiol (Mosk). 1976 Mar;21(3):71-3.
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Human pharmacokinetics of WR-2721.WR-2721的人体药代动力学。
Int J Radiat Oncol Biol Phys. 1986 Aug;12(8):1501-4. doi: 10.1016/0360-3016(86)90203-8.
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Binding of aminoalkylphosphorothioate radioprotective drugs to rodent tissue proteins.氨基烷基硫代磷酸酯辐射防护药物与啮齿动物组织蛋白的结合。
Biochem Pharmacol. 1990 Jun 1;39(11):1807-12. doi: 10.1016/0006-2952(90)90129-9.
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Variation in normal tissue responsiveness to WR-2721.
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Radiat Res. 1974 Aug;59(2):475-83.

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