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1
Antiviral activities of 9-R-2-phosphonomethoxypropyl adenine (PMPA) and bis(isopropyloxymethylcarbonyl)PMPA against various drug-resistant human immunodeficiency virus strains.9-R-2-膦酰甲氧基丙基腺嘌呤（PMPA）和双（异丙氧基甲基羰基）PMPA对多种耐药性人类免疫缺陷病毒株的抗病毒活性。
Antimicrob Agents Chemother. 1998 Jun;42(6):1484-7. doi: 10.1128/AAC.42.6.1484.
2
Anti-human immunodeficiency virus activity and cellular metabolism of a potential prodrug of the acyclic nucleoside phosphonate 9-R-(2-phosphonomethoxypropyl)adenine (PMPA), Bis(isopropyloxymethylcarbonyl)PMPA.无环核苷膦酸酯9-R-（2-膦酰甲氧基丙基）腺嘌呤（PMPA）的一种潜在前药双（异丙氧基甲基羰基）PMPA的抗人免疫缺陷病毒活性和细胞代谢
Antimicrob Agents Chemother. 1998 Mar;42(3):612-7. doi: 10.1128/AAC.42.3.612.
3
In vitro selection and characterization of HIV-1 with reduced susceptibility to PMPA.对替诺福韦酯敏感性降低的HIV-1的体外筛选与特性分析
Antivir Ther. 1999;4(2):87-94. doi: 10.1177/135965359900400205.
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Anti-HIV activity of adefovir (PMEA) and PMPA in combination with antiretroviral compounds: in vitro analyses.阿德福韦（PMEA）和替诺福韦酯与抗逆转录病毒化合物联合使用的抗HIV活性：体外分析
Antiviral Res. 1997 Nov;36(2):91-7. doi: 10.1016/s0166-3542(97)00043-0.
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Reversion of the M184V mutation in simian immunodeficiency virus reverse transcriptase is selected by tenofovir, even in the presence of lamivudine.即使在拉米夫定存在的情况下，替诺福韦也能选择出猿猴免疫缺陷病毒逆转录酶中M184V突变的回复突变。
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Tenofovir, adefovir, and zidovudine susceptibilities of primary human immunodeficiency virus type 1 isolates with non-B subtypes or nucleoside resistance.具有非B亚型或核苷类耐药性的原发性1型人类免疫缺陷病毒分离株对替诺福韦、阿德福韦和齐多夫定的敏感性
AIDS Res Hum Retroviruses. 2001 Aug 10;17(12):1167-73. doi: 10.1089/088922201316912772.
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Hydroxyurea enhances the activities of didanosine, 9-[2-(phosphonylmethoxy)ethyl]adenine, and 9-[2-(phosphonylmethoxy)propyl]adenine against drug-susceptible and drug-resistant human immunodeficiency virus isolates.羟基脲可增强去羟肌苷、9-[2-(膦酰甲氧基)乙基]腺嘌呤及9-[2-(膦酰甲氧基)丙基]腺嘌呤对药物敏感及耐药的人类免疫缺陷病毒分离株的活性。
Antimicrob Agents Chemother. 1999 Aug;43(8):2046-50. doi: 10.1128/AAC.43.8.2046.
9
Antiviral activity of tenofovir (PMPA) against nucleoside-resistant clinical HIV samples.
Nucleosides Nucleotides Nucleic Acids. 2001 Apr-Jul;20(4-7):1025-8. doi: 10.1081/NCN-100002483.
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Selective inhibition of HIV-1 reverse transcriptase by an antiviral inhibitor, (R)-9-(2-Phosphonylmethoxypropyl)adenine.一种抗病毒抑制剂（R）-9-（2-膦酰甲氧基丙基）腺嘌呤对HIV-1逆转录酶的选择性抑制作用
J Biol Chem. 1998 Oct 16;273(42):27250-8. doi: 10.1074/jbc.273.42.27250.

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Protection Against Rectal Chimeric Simian/Human Immunodeficiency Virus Transmission in Macaques by Rectal-Specific Gel Formulations of Maraviroc and Tenofovir.马拉维若和替诺福韦直肠特异性凝胶制剂对猕猴直肠嵌合型猿猴/人类免疫缺陷病毒传播的防护作用
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本文引用的文献

1
Anti-human immunodeficiency virus activity and cellular metabolism of a potential prodrug of the acyclic nucleoside phosphonate 9-R-(2-phosphonomethoxypropyl)adenine (PMPA), Bis(isopropyloxymethylcarbonyl)PMPA.无环核苷膦酸酯9-R-（2-膦酰甲氧基丙基）腺嘌呤（PMPA）的一种潜在前药双（异丙氧基甲基羰基）PMPA的抗人免疫缺陷病毒活性和细胞代谢
Antimicrob Agents Chemother. 1998 Mar;42(3):612-7. doi: 10.1128/AAC.42.3.612.
2
Antiretroviral therapy for HIV infection in 1997. Updated recommendations of the International AIDS Society-USA panel.1997年人类免疫缺陷病毒感染的抗逆转录病毒疗法。美国国际艾滋病学会小组的最新建议。
JAMA. 1997 Jun 25;277(24):1962-9.
3
In vitro induction of human immunodeficiency virus type 1 variants resistant to 2'-beta-Fluoro-2',3'-dideoxyadenosine.体外诱导对2'-β-氟-2',3'-二脱氧腺苷耐药的1型人类免疫缺陷病毒变体
Antimicrob Agents Chemother. 1997 Jun;41(6):1313-8. doi: 10.1128/AAC.41.6.1313.
4
Effects of (R)-9-(2-phosphonylmethoxypropyl)adenine monotherapy on chronic SIV infection in macaques.（R）-9-（2-膦酰甲氧基丙基）腺嘌呤单一疗法对猕猴慢性猴免疫缺陷病毒感染的影响。
AIDS Res Hum Retroviruses. 1997 May 20;13(8):707-12. doi: 10.1089/aid.1997.13.707.
5
Human immunodeficiency virus type 1 reverse transcriptase genotype and drug susceptibility changes in infected individuals receiving dideoxyinosine monotherapy for 1 to 2 years.接受双脱氧肌苷单药治疗1至2年的感染个体中1型人类免疫缺陷病毒逆转录酶基因型和药物敏感性的变化
Antimicrob Agents Chemother. 1997 Apr;41(4):757-62. doi: 10.1128/AAC.41.4.757.
6
9-[2-(Phosphonomethoxy)propyl]adenine therapy of established simian immunodeficiency virus infection in infant rhesus macaques.9-[2-(膦酰甲氧基)丙基]腺嘌呤对恒河猴幼猴已建立的猿猴免疫缺陷病毒感染的治疗
Antimicrob Agents Chemother. 1996 Nov;40(11):2586-91. doi: 10.1128/AAC.40.11.2586.
7
In vitro selection and molecular characterization of human immunodeficiency virus type 1 with reduced sensitivity to 9-[2-(phosphonomethoxy)ethyl]adenine (PMEA).对9-[2-(膦酰甲氧基)乙基]腺嘌呤（PMEA）敏感性降低的1型人类免疫缺陷病毒的体外筛选及分子特征分析
Antiviral Res. 1996 Oct;32(2):91-8. doi: 10.1016/0166-3542(95)00985-x.
8
Metabolism and in vitro antiretroviral activities of bis(pivaloyloxymethyl) prodrugs of acyclic nucleoside phosphonates.无环核苷膦酸双（新戊酰氧甲基）前药的代谢及体外抗逆转录病毒活性
Antimicrob Agents Chemother. 1993 Oct;37(10):2247-50. doi: 10.1128/AAC.37.10.2247.
9
Combination therapy with zidovudine and didanosine selects for drug-resistant human immunodeficiency virus type 1 strains with unique patterns of pol gene mutations.齐多夫定与去羟肌苷联合治疗会筛选出具有独特聚合酶基因（pol基因）突变模式的抗药性1型人类免疫缺陷病毒毒株。
J Infect Dis. 1994 Apr;169(4):722-9. doi: 10.1093/infdis/169.4.722.
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Characterization of human immunodeficiency virus type 1 mutants with decreased sensitivity to proteinase inhibitor Ro 31-8959.
Virology. 1995 Jan 10;206(1):527-34. doi: 10.1016/s0042-6822(95)80069-7.

9-R-2-膦酰甲氧基丙基腺嘌呤（PMPA）和双（异丙氧基甲基羰基）PMPA对多种耐药性人类免疫缺陷病毒株的抗病毒活性。

Antiviral activities of 9-R-2-phosphonomethoxypropyl adenine (PMPA) and bis(isopropyloxymethylcarbonyl)PMPA against various drug-resistant human immunodeficiency virus strains.

作者信息

Srinivas R V, Fridland A

机构信息

Department of Infectious Diseases, St. Jude Children's Research Hospital, Memphis, USA.

出版信息

Antimicrob Agents Chemother. 1998 Jun;42(6):1484-7. doi: 10.1128/AAC.42.6.1484.

DOI:10.1128/AAC.42.6.1484
PMID:9624498
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC105626/
Abstract

9-R-2-Phosphonomethoxypropyl adenine (PMPA) is an acyclic nucleoside phosphonate analog that has demonstrated efficacy against human immunodeficiency virus (HIV). We recently described the synthesis, metabolism, and biological activities of bis(isopropyloxymethylcarbonyl)PMPA [bis(poc)PMPA] as an orally bioavailable prodrug for PMPA. Among a large panel of drug-resistant HIV type 1 variants, only the K65R virus was resistant to PMPA. K65R virus also showed reduced susceptibility to bis(poc)PMPA, although the prodrug could still inhibit these viruses at submicromolar, nontoxic concentrations. Among a panel of seven primary clinical isolates from patients with diverse treatment histories, only one isolate showed reduced susceptibility to PMPA and was found to carry three mutations (M41L, T69N, R73K) in its reverse transcriptase catalytic domain.

摘要

9 - R - 2 - 膦酰甲氧基丙基腺嘌呤（PMPA）是一种无环核苷膦酸类似物，已证明对人类免疫缺陷病毒（HIV）有效。我们最近描述了双（异丙氧基甲基羰基）PMPA [双（poc）PMPA]作为PMPA的口服生物利用前药的合成、代谢和生物活性。在一大组耐药的1型HIV变体中，只有K65R病毒对PMPA耐药。K65R病毒对双（poc）PMPA的敏感性也降低，尽管该前药仍能在亚微摩尔无毒浓度下抑制这些病毒。在一组来自具有不同治疗史患者的7株原发性临床分离株中，只有1株对PMPA的敏感性降低，并且在其逆转录酶催化结构域中发现携带三个突变（M41L、T69N、R73K）。