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尿嘧啶类似物对1型人类免疫缺陷病毒及其逆转录酶的作用。

Action of uracil analogs on human immunodeficiency virus type 1 and its reverse transcriptase.

作者信息

Piras G, Dutschman G E, Im G J, Pan B C, Chu S H, Cheng Y C

机构信息

Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520, USA.

出版信息

Antimicrob Agents Chemother. 1995 Feb;39(2):539-41. doi: 10.1128/AAC.39.2.539.

DOI:10.1128/AAC.39.2.539
PMID:7537030
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC162575/
Abstract

Three structural analogs of 5-ethyl-1-benzyloxymethyl-6-(phenylthio)uracil (E-BPU) inhibited human immunodeficiency virus type 1 (HIV-1) replication without cytotoxicity in vitro and were more potent than azidothymidine and were as potent as E-BPU. The target of these compounds is HIV-1 reverse transcriptase. Reverse transcriptases resistant to nevirapine (tyrosine at position 181 to cysteine) and TIBO R82150 (leucine at position 100 to isoleucine) are cross resistant to E-BPU analogs. Nevirapine- or TIBO R82150-resistant HIV-1 were cross resistant to E-BPU analogs but were inhibited at concentrations 11- to 135-fold lower than the cytotoxic doses.

摘要

5-乙基-1-苄氧甲基-6-（苯硫基）尿嘧啶（E-BPU）的三种结构类似物在体外可抑制人类免疫缺陷病毒1型（HIV-1）复制且无细胞毒性，其效力比叠氮胸苷更强，与E-BPU效力相当。这些化合物的作用靶点是HIV-1逆转录酶。对奈韦拉平（第181位酪氨酸突变为半胱氨酸）和TIBO R82150（第100位亮氨酸突变为异亮氨酸）耐药的逆转录酶对E-BPU类似物存在交叉耐药性。对奈韦拉平或TIBO R82150耐药的HIV-1对E-BPU类似物也存在交叉耐药性，但在比细胞毒性剂量低11至135倍的浓度下受到抑制。

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本文引用的文献

1
A single conservative amino acid substitution in the reverse transcriptase of human immunodeficiency virus-1 confers resistance to (+)-(5S)-4,5,6,7-tetrahydro-5-methyl-6-(3-methyl-2-butenyl)imidazo[4,5, 1- jk][1,4]benzodiazepin-2(1H)-thione (TIBO R82150).人类免疫缺陷病毒1型逆转录酶中的单个保守氨基酸取代赋予了对（+）-（5S）-4,5,6,7-四氢-5-甲基-6-（3-甲基-2-丁烯基）咪唑并[4,5,1-jk][1,4]苯并二氮杂卓-2（1H）-硫酮（TIBO R82150）的抗性。
Mol Pharmacol. 1993 Jan;43(1):11-6.
2
HIV resistance to reverse transcriptase inhibitors.人类免疫缺陷病毒对逆转录酶抑制剂的耐药性。
Biochem Pharmacol. 1994 Jan 20;47(2):155-69. doi: 10.1016/0006-2952(94)90001-9.
3
Identification of the amino acid in the human immunodeficiency virus type 1 reverse transcriptase involved in the pyrophosphate binding of antiviral nucleoside triphosphate analogs and phosphonoformate. Implications for multiple drug resistance.
Biochem Pharmacol. 1993 Dec 14;46(12):2307-13. doi: 10.1016/0006-2952(93)90622-4.
4
Human immunodeficiency virus type 1 mutants resistant to nonnucleoside inhibitors of reverse transcriptase arise in tissue culture.在组织培养中出现了对逆转录酶非核苷抑制剂耐药的1型人类免疫缺陷病毒突变体。
Proc Natl Acad Sci U S A. 1991 Dec 15;88(24):11241-5. doi: 10.1073/pnas.88.24.11241.
5
Viral resistance to human immunodeficiency virus type 1-specific pyridinone reverse transcriptase inhibitors.对1型人类免疫缺陷病毒特异性吡啶酮逆转录酶抑制剂的病毒抗性。
J Virol. 1991 Sep;65(9):4887-92. doi: 10.1128/JVI.65.9.4887-4892.1991.
6
Pyridinone derivatives: specific human immunodeficiency virus type 1 reverse transcriptase inhibitors with antiviral activity.吡啶酮衍生物：具有抗病毒活性的特异性人类免疫缺陷病毒1型逆转录酶抑制剂
Proc Natl Acad Sci U S A. 1991 Aug 1;88(15):6863-7. doi: 10.1073/pnas.88.15.6863.
7
Highly potent and selective inhibition of human immunodeficiency virus type 1 by a novel series of 6-substituted acyclouridine derivatives.
Mol Pharmacol. 1991 Jun;39(6):805-10.
8
Inhibition of human immunodeficiency virus type 1 (HIV-1) replication by the dipyridodiazepinone BI-RG-587.二吡啶并二氮杂卓酮BI-RG-587对人类免疫缺陷病毒1型（HIV-1）复制的抑制作用
J Infect Dis. 1991 May;163(5):966-70. doi: 10.1093/infdis/163.5.966.
9
DNA polymerases versus HIV reverse transcriptase in AIDS therapy.
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