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1
Cell type-specific anti-human immunodeficiency virus type 1 activity of the transactivation inhibitor Ro5-3335.
Antimicrob Agents Chemother. 1992 Dec;36(12):2628-33. doi: 10.1128/AAC.36.12.2628.
2
Differential effect of tumor necrosis factor-alpha and herpes simplex virus type 1 on the Tat-targeted inhibition of human immunodeficiency virus type 1 replication.肿瘤坏死因子-α和1型单纯疱疹病毒对靶向Tat抑制1型人类免疫缺陷病毒复制的差异作用。
Virology. 1994 Aug 1;202(2):521-9. doi: 10.1006/viro.1994.1374.
3
2-Glycineamide-5-chlorophenyl 2-pyrryl ketone, a non-benzodiazepin Tat antagonist, is effective against acute and chronic HIV-1 infections in vitro.
Antiviral Res. 1996 Oct;32(2):55-62. doi: 10.1016/0166-3542(95)00980-9.
4
Inhibition of HIV replication in acute and chronic infections in vitro by a Tat antagonist.一种Tat拮抗剂在体外对急性和慢性感染中HIV复制的抑制作用。
Science. 1991 Dec 20;254(5039):1799-802. doi: 10.1126/science.1763331.
5
Inhibition of human immunodeficiency virus type 1 Tat-dependent activation of translation in Xenopus oocytes by the benzodiazepine Ro24-7429 requires trans-activation response element loop sequences.苯二氮䓬Ro24 - 7429对非洲爪蟾卵母细胞中人类免疫缺陷病毒1型Tat依赖的翻译激活的抑制作用需要反式激活应答元件环序列。
J Virol. 1994 Jan;68(1):25-33. doi: 10.1128/JVI.68.1.25-33.1994.
6
The human immunodeficiency virus type 1 Tat antagonist, Ro 5-3335, predominantly inhibits transcription initiation from the viral promoter.1型人类免疫缺陷病毒反式激活因子拮抗剂Ro 5-3335主要抑制病毒启动子的转录起始。
J Virol. 1995 Apr;69(4):2640-3. doi: 10.1128/JVI.69.4.2640-2643.1995.
7
Discovery and characterization of an HIV-1 Tat antagonist.一种HIV-1反式激活因子拮抗剂的发现与特性研究
Biochem Soc Trans. 1992 May;20(2):525-31. doi: 10.1042/bst0200525.
8
S-adenosylhomocysteine hydrolase inhibitors interfere with the replication of human immunodeficiency virus type 1 through inhibition of the LTR transactivation.S-腺苷同型半胱氨酸水解酶抑制剂通过抑制长末端重复序列（LTR）反式激活来干扰1型人类免疫缺陷病毒的复制。
Mol Pharmacol. 1997 Dec;52(6):1157-63. doi: 10.1124/mol.52.6.1157.
9
Interactions of thyroid hormone receptor with the human immunodeficiency virus type 1 (HIV-1) long terminal repeat and the HIV-1 Tat transactivator.甲状腺激素受体与人免疫缺陷病毒1型（HIV-1）长末端重复序列及HIV-1反式激活因子Tat的相互作用。
J Virol. 1995 Aug;69(8):5103-12. doi: 10.1128/JVI.69.8.5103-5112.1995.
10
Camptothecin inhibits Tat-mediated transactivation of type 1 human immunodeficiency virus.喜树碱抑制1型人类免疫缺陷病毒的Tat介导的反式激活。
J Biol Chem. 1994 Mar 11;269(10):7051-4.

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Targeted siRNA Delivery Against RUNX1 Via tFNA: Inhibiting Retinal Neovascularization and Restoring Vessels Through Dll4/Notch1 Signaling.通过经皮细针穿刺抽吸（tFNA）靶向递送针对RUNX1的小干扰RNA（siRNA）：通过Dll4/Notch1信号通路抑制视网膜新生血管形成并恢复血管
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Inhibition of human immunodeficiency virus type 1 replication in acutely and chronically infected cells by EM2487, a novel substance produced by a Streptomyces species.链霉菌属产生的一种新型物质EM2487对急性和慢性感染细胞中1型人类免疫缺陷病毒复制的抑制作用
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Potent and selective inhibition of human immunodeficiency virus type 1 transcription by piperazinyloxoquinoline derivatives.哌嗪基氧代喹啉衍生物对人免疫缺陷病毒1型转录的强效选择性抑制作用。
Antimicrob Agents Chemother. 1997 Jun;41(6):1250-5. doi: 10.1128/AAC.41.6.1250.
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SRR-SB3, a disulfide-containing macrolide that inhibits a late stage of the replicative cycle of human immunodeficiency virus.SRR-SB3，一种含二硫键的大环内酯类化合物，可抑制人类免疫缺陷病毒复制周期的晚期阶段。
Antimicrob Agents Chemother. 1997 Feb;41(2):262-8. doi: 10.1128/AAC.41.2.262.
7
Use of standardized SCID-hu Thy/Liv mouse model for preclinical efficacy testing of anti-human immunodeficiency virus type 1 compounds.使用标准化的SCID-hu Thy/Liv小鼠模型进行抗1型人类免疫缺陷病毒化合物的临床前疗效测试。
Antimicrob Agents Chemother. 1996 Mar;40(3):755-62. doi: 10.1128/AAC.40.3.755.
8
Inhibition of type 1 human immunodeficiency virus replication by a tat antagonist to which the virus remains sensitive after prolonged exposure in vitro.一种tat拮抗剂对1型人类免疫缺陷病毒复制的抑制作用，该病毒在体外长时间暴露后仍对其敏感。
Proc Natl Acad Sci U S A. 1993 Jul 15;90(14):6395-9. doi: 10.1073/pnas.90.14.6395.
9
Inhibition of human immunodeficiency virus type 1 Tat-dependent activation of translation in Xenopus oocytes by the benzodiazepine Ro24-7429 requires trans-activation response element loop sequences.苯二氮䓬Ro24 - 7429对非洲爪蟾卵母细胞中人类免疫缺陷病毒1型Tat依赖的翻译激活的抑制作用需要反式激活应答元件环序列。
J Virol. 1994 Jan;68(1):25-33. doi: 10.1128/JVI.68.1.25-33.1994.
10
An autoregulated dual-function antitat gene for human immunodeficiency virus type 1 gene therapy.一种用于人类免疫缺陷病毒1型基因治疗的自动调节双功能抗tat基因。
J Virol. 1995 Jan;69(1):206-12. doi: 10.1128/JVI.69.1.206-212.1995.

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CONTINUOUS CULTURE OF HUMAN LYMPHOBLASTS FROM PERIPHERAL BLOOD OF A CHILD WITH ACUTE LEUKEMIA.从一名急性白血病患儿外周血中连续培养人淋巴细胞
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Cell type-specific anti-human immunodeficiency virus type 1 activity of the transactivation inhibitor Ro5-3335.

作者信息

Witvrouw M, Pauwels R, Vandamme A M, Schols D, Reymen D, Yamamoto N, Desmyter J, De Clercq E

机构信息

Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium.

出版信息

Antimicrob Agents Chemother. 1992 Dec;36(12):2628-33. doi: 10.1128/AAC.36.12.2628.

DOI:10.1128/AAC.36.12.2628
PMID:1282790
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC245518/
Abstract

The drug Ro5-3335 [7-chloro-5-(2-pyrryl)-3H-1,4-benzodiazepin-2(H)-one] inhibits human immunodeficiency virus type 1 (HIV-1) gene expression at the transcriptional level through interference with Tat-mediated transactivation (M.-C. Hsu, A. D. Schutt, M. Holly, L. W. Slice, M. I. Sherman, D. D. Richman, M. J. Potash, and D. J. Volsky, Science 254:1799-1802, 1991). We confirmed this specific inhibitory effect in a quantitative bioassay based on transactivation of a chimeric gene comprising the HIV-1 long terminal repeat promoter fused to the lacZ gene of Escherichia coli and transfected in a HeLa cell line expressing Tat. Ro5-3335 was found to inhibit HIV-1 long terminal repeat-driven lacZ gene expression at a 50% inhibitory concentration of 0.5 microM. The in vitro anti-HIV-1 activity of Ro5-3335 was highly dependent on the nature of the host cells. The highest selectivity index, 50, was found in phytohemagglutinin-stimulated peripheral blood lymphocytes. The selectivity index was between 1 and 10 in the CD4+ T-cell lines CEM, MOLT-4 (clone 8), and HUT-78. In MT-4 and MT-2 cells, Ro5-3335 had no inhibitory effect on HIV-1 replication. The absence of anti-HIV-1 activity of Ro5-3335 in MT-4 cells was confirmed by using different parameters of virus replication and different multiplicities of infection. In persistently HIV-1-infected HUT-78/IIIB/LAI cells, Ro5-3335 failed to demonstrate any activity at subtoxic concentrations. The cytotoxicity of Ro5-3335 was significantly lower in peripheral blood lymphocytes than in the CD4+ T-cell lines.

摘要