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3-去氮尿苷(NSC 126849):一种有趣的生化反应调节剂。

3-Deazauridine (NSC 126849): an interesting modulator of biochemical response.

作者信息

Moriconi W J, Slavik M, Taylor S

出版信息

Invest New Drugs. 1986;4(1):67-84. doi: 10.1007/BF00172020.

Abstract

3-Deazauridine (NSC 126849) is a structural analog of uridine that inhibits the biosynthesis of Cytidine-5'-Triphosphate by competitive inhibition of Cytidine Triphosphate synthetase which is considered to be the primary mode of action of this nucleoside analog. Despite a paucity of clinical attention given to this drug as a single agent, it has generated much enthusiasm as a biological response modulator because of its synergistic effect with a number of antitumor agents including Cytosine Arabinoside, 5-aza-2'-deoxycytidine, 5-azacytidine, thymidine and D-galactosamine, although only the cytosine arabinoside/3-Deazauridine combination has been explored clinically. In this paper, the current status of the drug and future perspectives will be discussed.

摘要

3-去氮尿苷(NSC 126849)是尿苷的结构类似物,它通过竞争性抑制胞苷三磷酸合成酶来抑制胞苷-5'-三磷酸的生物合成,这被认为是这种核苷类似物的主要作用方式。尽管作为单一药物时该药物很少受到临床关注,但由于它与多种抗肿瘤药物(包括阿糖胞苷、5-氮杂-2'-脱氧胞苷、5-氮杂胞苷、胸腺嘧啶核苷和D-半乳糖胺)具有协同作用,作为一种生物反应调节剂已引起了广泛关注,不过只有阿糖胞苷/3-去氮尿苷组合进行了临床研究。本文将讨论该药物的现状和未来前景。

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