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早期核苷逆转录酶抑制剂治疗 HIV:司他夫定(D4T)的简史及其与其他双脱氧核苷的比较。

Early nucleoside reverse transcriptase inhibitors for the treatment of HIV: a brief history of stavudine (D4T) and its comparison with other dideoxynucleosides.

机构信息

Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, United States.

出版信息

Antiviral Res. 2010 Jan;85(1):34-8. doi: 10.1016/j.antiviral.2009.10.006. Epub 2009 Oct 23.

DOI:10.1016/j.antiviral.2009.10.006
PMID:19854224
Abstract

The occasion of this 25th anniversary issue encouraged us to reminisce about the important history of the discovery of the dideoxynucleoside analogues for the treatment of HIV/AIDS and to chronicle our thoughts about a particular exciting and rewarding period of our scientific careers. Following the identification of the anti-HIV activity of zidovudine (AZT), we participated in the urgent quest to discover optimal treatments of HIV infection and AIDS. A number of previously synthesized nucleoside analogues were comparatively evaluated, and stavudine (D4T) emerged as a promising candidate for development. Following clinical evaluation, D4T became a mainstay of the initial antiretroviral combination therapy, prolonging and saving numerous lives. It has only recently been supplanted by better-tolerated treatments. This article forms part of a special issue of Antiviral Research marking the 25th anniversary of antiretroviral drug discovery and development, vol. 85, issue 1, 2010.

摘要

本期 25 周年特刊促使我们回忆起发现用于治疗 HIV/AIDS 的双脱氧核苷类似物的重要历史,并记录下我们对职业生涯中这一激动人心、收获颇丰的特殊时期的一些想法。在鉴定齐多夫定(AZT)的抗 HIV 活性后,我们参与了寻找 HIV 感染和艾滋病最佳治疗方法的紧急探索。对多种先前合成的核苷类似物进行了比较评估, stavudine(D4T)脱颖而出成为有开发前景的候选药物。经过临床评估,D4T 成为最初抗逆转录病毒联合疗法的基础,延长并挽救了众多生命。直到最近,它才被耐受性更好的治疗方法所取代。本文是抗病毒研究特刊的一部分,该特刊是为了纪念抗逆转录病毒药物发现和开发 25 周年,第 85 卷,第 1 期,2010 年。

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