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嘌呤核苷类似物的代谢与作用

Metabolism and action of purine nucleoside analogs.

作者信息

Plunkett W, Saunders P P

机构信息

Department of Medical Oncology, University of Texas M.D. Anderson Cancer Center, Houston 77030.

出版信息

Pharmacol Ther. 1991;49(3):239-68. doi: 10.1016/0163-7258(91)90057-s.

Abstract

Recent investigations have identified many new purine nucleoside analogs that act as antimetabolites. This article focuses on the metabolism and mechanisms of action of tiazofurin, 3-deazaguanosine, neplanocin A, arabinosyladenine in combination with inhibitors of adenosine deaminase, arabinosyl-2-fluoroadenine, and 2-chloro-2'-deoxyadenosine, drugs that are either currently being evaluated in clinical trials or are close to that stage. The diverse metabolic requirements for activation, unique mechanisms of action, and differential biological activities of these compounds are characterized and evaluated for prospective therapeutic application.

摘要

最近的研究已经鉴定出许多作为抗代谢物的新型嘌呤核苷类似物。本文重点关注硫唑嘌呤、3-脱氮鸟苷、奈拉滨、与腺苷脱氨酶抑制剂联合使用的阿糖腺苷、阿糖基-2-氟腺苷和2-氯-2'-脱氧腺苷的代谢及作用机制,这些药物要么目前正在进行临床试验评估,要么已接近该阶段。对这些化合物激活所需的不同代谢条件、独特的作用机制和不同的生物学活性进行了表征和评估,以用于前瞻性治疗应用。

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