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天然产物抑制剂对 HIV-1 逆转录酶、蛋白酶和整合酶的抑制作用。

Inhibitors from natural products to HIV-1 reverse transcriptase, protease and integrase.

机构信息

Center for AIDS Research, Nankai University, Tianjin, China.

出版信息

Mini Rev Med Chem. 2010 Dec;10(14):1331-44. doi: 10.2174/138955710793564133.

DOI:10.2174/138955710793564133
PMID:21175425
Abstract

Acquired immunodeficiency syndrome (AIDS), caused by human immunodeficiency virus type 1 (HIV-1) infection, is still one of the most challenging diseases of the early 21st century. Reverse transcriptase (RT), protease (PR) and integrase (IN) are three key enzymes of HIV-1. Despite the shortcomings of chemical drugs such as toxicity, lack of curative and multiple effects, the search for more and better anti-HIV agents has been focused on natural products. Many natural products have been shown to possess promising activities that could assist in the prevention and amelioration of the disease. Most of these natural anti-HIV agents have other medicinal values as well, which afford them further prospective as novel lead compounds for the development of new drugs. These natural products can deal with both the virus and the various disorders that are caused by HIV. In this review, natural inhibitors of RT, PR and IN have been found to be classified and the relationship between structure and inhibitory activity is discussed.

摘要

获得性免疫缺陷综合征(AIDS),由人类免疫缺陷病毒 1 型(HIV-1)感染引起,仍然是 21 世纪早期最具挑战性的疾病之一。逆转录酶(RT)、蛋白酶(PR)和整合酶(IN)是 HIV-1 的三种关键酶。尽管化学药物存在毒性、缺乏疗效和多种作用等缺点,但人们仍专注于寻找更多更好的抗 HIV 药物,这些药物来自天然产物。许多天然产物已被证明具有有前途的活性,可以帮助预防和改善这种疾病。这些天然抗 HIV 药物中的大多数也具有其他药用价值,这使它们有希望成为开发新药的新型先导化合物。这些天然产物可以同时处理病毒和 HIV 引起的各种疾病。在这篇综述中,发现了 RT、PR 和 IN 的天然抑制剂,并对其进行了分类,讨论了结构与抑制活性之间的关系。

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