Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV
Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV
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DOI：
10.1016/j.bmc.2007.09.010
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发表时间：
2007-12-15
影响因子：
3.5
通讯作者：
Mitsuya, Hiroaki
中科院分区：
文献类型：
--
作者：
Ghosh, Arun K.;Dawson, Zachary L.;Mitsuya, Hiroaki
我们基于结构的设计策略。靶向HIV-1蛋白酶主干，产生了许多非常有效的非肽基抑制剂。其中一种抑制剂darunavir （TMC114）含有一个特殊的、基于结构设计的高亲和P2配体，3(R), 3a(S), 6a(R)双-四氢呋喃脲（bis-THF）。Darunavir最近被批准用于治疗HIV-1多药耐药患者，这些患者对先前存在的HAART治疗方案没有反应。(c) 2007 Elsevier Ltd.版权所有。
Our structure-based design strategies which specifi. cally target the HIV-1 protease backbone, resulted in a number of exceedingly potent nonpeptidyl inhibitors. One of these inhibitors, darunavir (TMC114), contains a privileged, structure-based designed high-affinity P2 ligand, 3(R), 3a(S), 6a(R) bis-tetrahydrofuranylurethane (bis-THF). Darunavir has recently been approved for the treatment of HIV/AIDS patients harboring multidrug-resistant HIV-1 variants that do not respond to previously existing HAART regimens. (c) 2007 Elsevier Ltd. All rights reserved.