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9-β-D-阿拉伯呋喃糖基-2-氟腺嘌呤掺入HL-60细胞的RNA和DNA中。

Incorporation of 9-beta-D-arabinofuranosyl-2-fluoroadenine into HL-60 cellular RNA and DNA.

作者信息

Spriggs D, Robbins G, Mitchell T, Kufe D

出版信息

Biochem Pharmacol. 1986 Jan 15;35(2):247-52. doi: 10.1016/0006-2952(86)90521-6.

Abstract

The incorporation of 9-beta-D-arabinofuranosyl-2-fluoroadenine (F-ara-A) into HL-60 cellular nucleic acids was monitored by cesium sulfate gradient centrifugation. The results demonstrated that F-ara-A incorporated into both RNA and DNA. These findings are in contrast to those previously obtained with 1-beta-D-arabinofuranosylcytosine (ara-C) and 9-beta-arabinofuranosyladenine (ara-A) which demonstrated incorporation of these nucleosides only in DNA. F-ara-A inhibited HL-60 proliferation, and the incorporation of F-ara-A into both DNA and RNA correlated with loss of clonogenic survival. Furthermore, cytostatic concentrations of F-ara-A resulted in the appearance of a more mature phenotype, a finding consistent with the effects of other inhibitors of DNA synthesis. The incorporation of F-ara-A into RNA and DNA should provide new insights regarding the mechanism of action of this agent.

摘要

通过硫酸铯梯度离心法监测9-β-D-阿拉伯呋喃糖基-2-氟腺嘌呤(F-ara-A)掺入HL-60细胞核酸的情况。结果表明,F-ara-A可掺入RNA和DNA。这些发现与先前用1-β-D-阿拉伯呋喃糖基胞嘧啶(ara-C)和9-β-阿拉伯呋喃糖基腺嘌呤(ara-A)所获得的结果相反,先前的结果表明这些核苷仅掺入DNA。F-ara-A抑制HL-60细胞增殖,且F-ara-A掺入DNA和RNA均与克隆形成存活率的丧失相关。此外,F-ara-A的细胞生长抑制浓度导致出现更成熟的表型,这一发现与其他DNA合成抑制剂的作用效果一致。F-ara-A掺入RNA和DNA应为该药物的作用机制提供新的见解。

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