Kappa-opioid receptor agonist suppression of HIV-1 expression in CD4+ lymphocytes.
Kappa-opioid receptor agonist suppression of HIV-1 expression in CD4+ lymphocytes.
复制标题
Kappa-阿片受体激动剂抑制 CD4 淋巴细胞中 HIV-1 的表达。
DOI：
10.1016/s0006-2952(01)00574-3
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发表时间：
2001
影响因子：
5.8
通讯作者：
Portoghese,PS
中科院分区：
文献类型：
--
作者：
Peterson,PK;Gekker,G;Lokensgard,JR;Bidlack,JM;Chang,AC;Fang,X;Portoghese,PS
Synthetic κ-opioid receptor (KOR) agonists have been shown to suppress HIV-1 expression in acutely infected macrophages. In the present study, we examined the effects of the KOR ligand trans-3,4-dichloro-N-methyl-N[2-(1-pyrolidinyl)cyclohexyl]benzeneaceamide methanesulfonate (U50,488) on HIV-1 expression in CD4+lymphocytes, the main target cell of this virus. When U50,488 was added to activated CD4+lymphocytes, HIV-1 expression was inhibited in a concentration- and time-dependent manner with maximal suppression (≈60%) at 10-7M U50,488. The KOR selective antagonist nor-binaltorphimine (nor-BNI) had no effect by itself on viral expression but blocked the antiviral property of U50,488, suggesting that U50,488 was acting via a KOR-related mechanism. Support for the involvement of KOR was provided by the findings that 34% of activated CD4+lymphocytes were positive for KOR, using an immunofluorescence technique, and that seven additional synthetic KOR ligands also inhibited HIV-1 expression. The results of this study broaden understanding of the antiviral properties of KOR ligands to include cells outside of the nervous system and suggest a potential role for these agents in the treatment of HIV-1 infection.
