胸苷和尿苷对人单核细胞中3'-叠氮-3'-脱氧胸苷（齐多夫定）磷酸化的影响。
Effects of thymidine and uridine on the phosphorylation of 3'-azido-3'-deoxythymidine (zidovudine) in human mononuclear cells.
作者信息
Szebeni J, Patel S S, Hung K, Wahl L M, Weinstein J N
机构信息
National Cancer Institute, Bethesda, Maryland 20892.
出版信息
Antimicrob Agents Chemother. 1991 Jan;35(1):198-200. doi: 10.1128/AAC.35.1.198.
Abstract
The effects of thymidine and uridine on the phosphorylation of 3'-azido-3'-deoxythymidine (AZT) were studied in various human mononuclear cell preparations. Thymidine suppressed [3H]AZT phosphorylation in the same concentration range (20 to 100 microM) in which it antagonizes the anti-human immunodeficiency virus activity of AZT. Uridine, in turn, had no influence on AZT phosphorylation, just as it has no effect on the anti-human immunodeficiency virus activity of AZT. These findings are consistent with a close relationship between the inhibition of AZT phosphorylation and the influence of physiological nucleosides on the antiviral activity of AZT.
摘要
在多种人类单核细胞制剂中研究了胸苷和尿苷对3'-叠氮-3'-脱氧胸苷（AZT）磷酸化的影响。胸苷在20至100微摩尔的相同浓度范围内抑制[3H]AZT磷酸化，在此浓度范围内它拮抗AZT的抗人类免疫缺陷病毒活性。相反，尿苷对AZT磷酸化没有影响，就像它对AZT的抗人类免疫缺陷病毒活性没有影响一样。这些发现与AZT磷酸化的抑制和生理核苷对AZT抗病毒活性的影响之间的密切关系是一致的。
相似文献
1
Effects of thymidine and uridine on the phosphorylation of 3'-azido-3'-deoxythymidine (zidovudine) in human mononuclear cells.胸苷和尿苷对人单核细胞中3'-叠氮-3'-脱氧胸苷（齐多夫定）磷酸化的影响。
Antimicrob Agents Chemother. 1991 Jan;35(1):198-200. doi: 10.1128/AAC.35.1.198.
2
Uridine reverses the toxicity of 3'-azido-3'-deoxythymidine in normal human granulocyte-macrophage progenitor cells in vitro without impairment of antiretroviral activity.尿苷可在体外逆转3'-叠氮-3'-脱氧胸苷对正常人粒细胞-巨噬细胞祖细胞的毒性，且不损害其抗逆转录病毒活性。
Antimicrob Agents Chemother. 1988 Jul;32(7):997-1001. doi: 10.1128/AAC.32.7.997.
3
4
Long-term exposure to zidovudine affects in vitro and in vivo the efficiency of phosphorylation of thymidine kinase.
AIDS Res Hum Retroviruses. 1996 Feb 10;12(3):223-8. doi: 10.1089/aid.1996.12.223.
5
Effect of dipyridamole on transport and phosphorylation of thymidine and 3'-azido-3'-deoxythymidine in human monocyte/macrophages.
Biochem Pharmacol. 1990 Aug 15;40(4):867-70. doi: 10.1016/0006-2952(90)90328-i.
6
Amino acid phosphoramidate monoesters of 3'-azido-3'-deoxythymidine: relationship between antiviral potency and intracellular metabolism.3'-叠氮-3'-脱氧胸苷的氨基酸磷酰胺单酯：抗病毒效力与细胞内代谢之间的关系。
J Med Chem. 2001 Jan 18;44(2):223-31. doi: 10.1021/jm000260r.
7
Comparison of rates of intracellular metabolism of zidovudine in human and primate peripheral blood mononuclear cells.齐多夫定在人和灵长类动物外周血单核细胞内代谢速率的比较。
Antimicrob Agents Chemother. 1994 Oct;38(10):2398-403. doi: 10.1128/AAC.38.10.2398.
8
Alteration of thymidine kinase activity in cells treated with an antiviral agent.用抗病毒剂处理的细胞中胸苷激酶活性的改变。
J Biol Regul Homeost Agents. 1995 Apr-Jun;9(2):47-51.
9
Comparisons of anti-human immunodeficiency virus activities, cellular transport, and plasma and intracellular pharmacokinetics of 3'-fluoro-3'-deoxythymidine and 3'-azido-3'-deoxythymidine.3'-氟-3'-脱氧胸苷与3'-叠氮-3'-脱氧胸苷的抗人免疫缺陷病毒活性、细胞转运以及血浆和细胞内药代动力学比较
Antimicrob Agents Chemother. 1992 Apr;36(4):808-18. doi: 10.1128/AAC.36.4.808.
10
Catabolism of 3'-azido-3'-deoxythymidine in hepatocytes and liver microsomes, with evidence of formation of 3'-amino-3'-deoxythymidine, a highly toxic catabolite for human bone marrow cells.3'-叠氮-3'-脱氧胸苷在肝细胞和肝微粒体中的分解代谢，有证据表明形成了3'-氨基-3'-脱氧胸苷，这是一种对人类骨髓细胞具有高度毒性的分解代谢产物。
Mol Pharmacol. 1991 Feb;39(2):258-66.
引用本文的文献
1
Cellular pharmacology and potency of HIV-1 nucleoside analogs in primary human macrophages.HIV-1 核苷类似物在原代人巨噬细胞中的细胞药理学和效力。
Antimicrob Agents Chemother. 2013 Mar;57(3):1262-9. doi: 10.1128/AAC.02012-12. Epub 2012 Dec 21.
2
Substrate specificity and phosphorylation of antiviral and anticancer nucleoside analogues by human deoxyribonucleoside kinases and ribonucleoside kinases.人脱氧核糖核苷激酶和核糖核苷激酶对抗病毒和抗癌核苷类似物的底物特异性及磷酸化作用
Pharmacol Ther. 2003 Nov;100(2):119-39. doi: 10.1016/j.pharmthera.2003.07.001.
3
Mechanisms of nucleoside analog antiviral activity and resistance during human immunodeficiency virus reverse transcription.人类免疫缺陷病毒逆转录过程中核苷类似物抗病毒活性及耐药性的机制
Antimicrob Agents Chemother. 1996 Mar;40(3):527-40. doi: 10.1128/AAC.40.3.527.
4
Effects of dideoxyinosine and dideoxycytidine on the intracellular phosphorylation of zidovudine in human mononuclear cells.双脱氧肌苷和双脱氧胞苷对人单核细胞中齐多夫定细胞内磷酸化作用的影响。
Br J Clin Pharmacol. 1994 Oct;38(4):323-8. doi: 10.1111/j.1365-2125.1994.tb04361.x.
5
Drug interactions with zidovudine phosphorylation in vitro.齐多夫定磷酸化的体外药物相互作用。
Antimicrob Agents Chemother. 1995 Jun;39(6):1376-8. doi: 10.1128/AAC.39.6.1376.
6
Quantitative assay for testing susceptibility of HIV isolates to zidovudine and sCD4 (178)-PE40.用于检测HIV分离株对齐多夫定和sCD4(178)-PE40敏感性的定量测定
Eur J Clin Microbiol Infect Dis. 1992 Aug;11(8):715-21. doi: 10.1007/BF01989976.
本文引用的文献
1
THE DIFFERENTIATION OF MONONUCLEAR PHAGOCYTES. MORPHOLOGY, CYTOCHEMISTRY, AND BIOCHEMISTRY.单核吞噬细胞的分化。形态学、细胞化学与生物化学
J Exp Med. 1965 Jan 1;121(1):153-70. doi: 10.1084/jem.121.1.153.
2
Deoxycytidine excretion by mouse peritoneal macrophages: its implication in modulation of immunological functions.小鼠腹腔巨噬细胞的脱氧胞苷排泄：其在免疫功能调节中的意义。
J Cell Physiol. 1982 Apr;111(1):28-32. doi: 10.1002/jcp.1041110106.
3
Production of the effector molecule thymidine by human lung alveolar macrophages.
Eur J Cancer Clin Oncol. 1984 Dec;20(12):1543-8. doi: 10.1016/0277-5379(84)90148-2.
4
Isolation of human mononuclear cell subsets by counterflow centrifugal elutriation (CCE). II. Functional properties of B-lymphocyte-, T-lymphocyte-, and monocyte-enriched fractions.
Cell Immunol. 1984 May;85(2):384-95. doi: 10.1016/0008-8749(84)90252-1.
5
Isolation of human mononuclear cell subsets by counterflow centrifugal elutriation (CCE). I. Characterization of B-lymphocyte-, T-lymphocyte-, and monocyte-enriched fractions by flow cytometric analysis.通过逆流离心淘析法（CCE）分离人单核细胞亚群。I. 利用流式细胞术分析对富含B淋巴细胞、T淋巴细胞和单核细胞的组分进行表征。
Cell Immunol. 1984 May;85(2):373-83. doi: 10.1016/0008-8749(84)90251-x.
6
Structure-activity analysis of antagonism of the feedback inhibition of thymidine kinase.胸苷激酶反馈抑制拮抗作用的构效分析
Biochem Pharmacol. 1988 Apr 1;37(7):1293-8. doi: 10.1016/0006-2952(88)90785-x.
7
Uridine reverses the toxicity of 3'-azido-3'-deoxythymidine in normal human granulocyte-macrophage progenitor cells in vitro without impairment of antiretroviral activity.尿苷可在体外逆转3'-叠氮-3'-脱氧胸苷对正常人粒细胞-巨噬细胞祖细胞的毒性，且不损害其抗逆转录病毒活性。
Antimicrob Agents Chemother. 1988 Jul;32(7):997-1001. doi: 10.1128/AAC.32.7.997.
8
Quantitative immunocytofluorographic analysis of CD4 surface antigen expression and HIV infection of human peripheral blood monocyte/macrophages.人外周血单核细胞/巨噬细胞CD4表面抗原表达及HIV感染的定量免疫细胞荧光分析
AIDS Res Hum Retroviruses. 1987 Summer;3(2):135-45. doi: 10.1089/aid.1987.3.135.
9
Failure of dideoxynucleosides to inhibit human immunodeficiency virus replication in cultured human macrophages.双脱氧核苷在培养的人巨噬细胞中无法抑制人类免疫缺陷病毒复制。
J Exp Med. 1987 Oct 1;166(4):1144-9. doi: 10.1084/jem.166.4.1144.
Zotero 插件