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Sensitivity of (138 Glu-->Lys) mutated human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) to HIV-1-specific RT inhibitors.

作者信息

Balzarini J, Kleim J P, Riess G, Camarasa M J, De Clercq E, Karlsson A

机构信息

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

出版信息

Biochem Biophys Res Commun. 1994 Jun 30;201(3):1305-12. doi: 10.1006/bbrc.1994.1846.

DOI:10.1006/bbrc.1994.1846
PMID:7517668
Abstract

Human immunodeficiency virus type 1 (HIV-1) recombinant reverse transcriptase (RT) containing lysine (Lys) instead of glutamic acid (Glu) at position 138 proved fully resistant to the inhibitory effect of TSAO derivatives, but retained marked sensitivity to all other HIV-1-specific inhibitors investigated. In contrast, 181 Tyr-->Cys mutated RT lost sensitivity to all HIV-1-specific inhibitors. There was a close correlation between the sensitivity/resistance pattern of HIV-1-specific inhibitors against mutated (138 Glu-->Lys) recombinant HIV-1 RT and mutant virus strains selected for resistance against TSAO-m3T in cell culture and proven to contain the 138-Lys mutation as the sole mutation within the amino acid 50-270 region of their RT.

摘要

相似文献

1
Sensitivity of (138 Glu-->Lys) mutated human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) to HIV-1-specific RT inhibitors.
Biochem Biophys Res Commun. 1994 Jun 30;201(3):1305-12. doi: 10.1006/bbrc.1994.1846.
2
Human immunodeficiency virus type 1 (HIV-1) strains selected for resistance against the HIV-1-specific [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro- 5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)]-beta-D-pentofurano syl (TSAO) nucleoside analogues retain sensitivity to HIV-1-specific nonnucleoside inhibitors.针对HIV-1特异性[2',5'-双-O-(叔丁基二甲基甲硅烷基)-3'-螺-5''-(4''-氨基-1'',2''-氧硫杂环戊烯-2'',2''-二氧化物)]-β-D-戊呋喃糖基（TSAO）核苷类似物产生耐药性的1型人类免疫缺陷病毒（HIV-1）毒株，对HIV-1特异性非核苷抑制剂仍保持敏感。
Proc Natl Acad Sci U S A. 1993 Aug 1;90(15):6952-6. doi: 10.1073/pnas.90.15.6952.
3
Site-directed mutagenesis of human immunodeficiency virus type 1 reverse transcriptase at amino acid position 138.对人类免疫缺陷病毒1型逆转录酶第138位氨基酸进行定点诱变。
Virology. 2001 Feb 1;280(1):97-106. doi: 10.1006/viro.2000.0742.
4
Treatment of human immunodeficiency virus type 1 (HIV-1)-infected cells with combinations of HIV-1-specific inhibitors results in a different resistance pattern than does treatment with single-drug therapy.用1型人类免疫缺陷病毒（HIV-1）特异性抑制剂组合治疗HIV-1感染的细胞，会产生与单药治疗不同的耐药模式。
J Virol. 1993 Sep;67(9):5353-9. doi: 10.1128/JVI.67.9.5353-5359.1993.
5
Resistance of HIV-1 reverse transcriptase against [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro-5''-(4''-amino-1'',2''- oxathiole-2'',2''-dioxide)] (TSAO) derivatives is determined by the mutation Glu138-->Lys on the p51 subunit.HIV-1逆转录酶对[2',5'-双-O-(叔丁基二甲基甲硅烷基)-3'-螺-5''-(4''-氨基-1'',2''-氧硫杂环戊烯-2'',2''-二氧化物)]（TSAO）衍生物的耐药性由p51亚基上的Glu138→Lys突变决定。
J Biol Chem. 1994 Oct 14;269(41):25255-8.
6
Human immunodeficiency virus 1 (HIV-1)-specific reverse transcriptase (RT) inhibitors may suppress the replication of specific drug-resistant (E138K)RT HIV-1 mutants or select for highly resistant (Y181C-->C181I)RT HIV-1 mutants.人类免疫缺陷病毒1型（HIV-1）特异性逆转录酶（RT）抑制剂可能会抑制特定耐药性（E138K）RT HIV-1突变体的复制，或筛选出高耐药性（Y181C→C181I）RT HIV-1突变体。
Proc Natl Acad Sci U S A. 1994 Jul 5;91(14):6599-603. doi: 10.1073/pnas.91.14.6599.
7
Suppression of the breakthrough of human immunodeficiency virus type 1 (HIV-1) in cell culture by thiocarboxanilide derivatives when used individually or in combination with other HIV-1-specific inhibitors (i.e., TSAO derivatives).硫代羧酰苯胺衍生物单独使用或与其他HIV-1特异性抑制剂（即TSAO衍生物）联合使用时对细胞培养中1型人类免疫缺陷病毒（HIV-1）突破的抑制作用。
Proc Natl Acad Sci U S A. 1995 Jun 6;92(12):5470-4. doi: 10.1073/pnas.92.12.5470.
8
Human immunodeficiency virus type 1-specific [2',5'-bis-O-(tert- butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"- oxathiole-2",2"-dioxide)-purine analogues show a resistance spectrum that is different from that of the human immunodeficiency virus type 1-specific non-nucleoside analogues.1型人类免疫缺陷病毒特异性的[2',5'-双-O-(叔丁基二甲基甲硅烷基)-β-D-呋喃核糖基]-3'-螺-5"-(4"-氨基-1",2"-氧硫杂环戊二烯-2",2"-二氧化物)-嘌呤类似物显示出与1型人类免疫缺陷病毒特异性非核苷类似物不同的耐药谱。
Mol Pharmacol. 1993 Jan;43(1):109-14.
9
HIV-1-specific reverse transcriptase inhibitors show differential activity against HIV-1 mutant strains containing different amino acid substitutions in the reverse transcriptase.HIV-1特异性逆转录酶抑制剂对逆转录酶中含有不同氨基酸取代的HIV-1突变株表现出不同的活性。
Virology. 1993 Jan;192(1):246-53. doi: 10.1006/viro.1993.1027.
10
Resistance pattern of human immunodeficiency virus type 1 reverse transcriptase to quinoxaline S-2720.1型人类免疫缺陷病毒逆转录酶对喹喔啉S-2720的耐药模式
J Virol. 1994 Dec;68(12):7986-92. doi: 10.1128/JVI.68.12.7986-7992.1994.

引用本文的文献

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Subunit-selective mutational analysis and tissue culture evaluations of the interactions of the E138K and M184I mutations in HIV-1 reverse transcriptase.E138K 和 M184I 突变在 HIV-1 逆转录酶中的相互作用的亚单位选择性突变分析和组织培养评估。
J Virol. 2012 Aug;86(16):8422-31. doi: 10.1128/JVI.00271-12. Epub 2012 May 23.