非核苷类逆转录酶抑制剂UC-781和TMC120-R147681作为人类免疫缺陷病毒杀微生物剂的体外评价
In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides.
作者信息
Van Herrewege Yven, Michiels Jo, Van Roey Jens, Fransen Katrien, Kestens Luc, Balzarini Jan, Lewi Paul, Vanham Guido, Janssen Paul
机构信息
Laboratory of Immunology, Institute of Tropical Medicine, Antwerp, Belgium.
出版信息
Antimicrob Agents Chemother. 2004 Jan;48(1):337-9. doi: 10.1128/AAC.48.1.337-339.2004.
Abstract
The nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 (Dapivirine) effectively prevented human immunodeficiency virus (HIV) infection in cocultures of monocyte-derived dendritic cells and T cells, representing primary targets in sexual transmission. Both drugs had a favorable therapeutic index. A 24-h treatment with 1,000 nM UC-781 or 100 nM TMC120-R147681 prevented cell-free HIV infection, whereas 10-fold-higher concentrations blocked cell-associated HIV.
摘要
非核苷类逆转录酶抑制剂UC-781和TMC120-R147681（地瑞那韦）在单核细胞衍生的树突状细胞与T细胞的共培养物中能有效预防人类免疫缺陷病毒（HIV）感染，而这两种细胞是性传播中的主要靶细胞。这两种药物都具有良好的治疗指数。用1000 nM的UC-781或100 nM的TMC120-R147681进行24小时治疗可预防无细胞HIV感染，而浓度高出10倍时则可阻断细胞相关的HIV感染。
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本文引用的文献
1
Inhibition of vaginal transmission of HIV-1 in hu-SCID mice by the non-nucleoside reverse transcriptase inhibitor TMC120 in a gel formulation.
AIDS. 2003 Jul 25;17(11):1597-604. doi: 10.1097/00002030-200307250-00003.
2
Activity of reverse transcriptase inhibitors in monocyte-derived dendritic cells: a possible in vitro model for postexposure prophylaxis of sexual HIV transmission.
AIDS Res Hum Retroviruses. 2002 Oct 10;18(15):1091-102. doi: 10.1089/088922202320567833.
3
Attenuated infectivity of HIV type 1 from epithelial cells pretreated with a tight-binding nonnucleoside reverse transcriptase inhibitor.
AIDS Res Hum Retroviruses. 2002 Jul 1;18(10):711-4. doi: 10.1089/088922202760072339.
4
Considerations and development of topical microbicides to inhibit the sexual transmission of HIV.
Expert Opin Investig Drugs. 2002 Aug;11(8):1077-97. doi: 10.1517/13543784.11.8.1077.
5
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
Bioorg Med Chem Lett. 2001 Sep 3;11(17):2235-9. doi: 10.1016/s0960-894x(01)00412-7.
6
Long-term exposure of HIV type 1-infected cell cultures to combinations of the novel quinoxaline GW420867X with lamivudine, abacavir, and a variety of nonnucleoside reverse transcriptase inhibitors.
AIDS Res Hum Retroviruses. 2000 Apr 10;16(6):517-28. doi: 10.1089/088922200308936.
7
PCR-Based assay to quantify human immunodeficiency virus type 1 DNA in peripheral blood mononuclear cells.
J Clin Microbiol. 2000 Feb;38(2):630-4. doi: 10.1128/JCM.38.2.630-634.2000.
8
Sexual transmission of HIV: infectiousness and prevention.
AIDS. 1999 Feb 4;13(2):155-66. doi: 10.1097/00002030-199902040-00003.
9
Correlation of human immunodeficiency virus type 1 RNA levels in blood and the female genital tract.
J Infect Dis. 1999 Apr;179(4):871-82. doi: 10.1086/314656.
10
Observations from the CDC. The urgent need for new HIV/STD prevention options for women.
J Womens Health. 1998 Nov;7(9):1081-6. doi: 10.1089/jwh.1998.7.1081.
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