No cross-resistance or selection of HIV-1 resistant mutants in vitro to the antiretroviral tripeptide glycyl-prolyl-glycine-amide

被引：7

作者：

Andersson, E ^{[1
]}

Horal, P

Vahne, A

Svennerholm, B

机构：

[1] Gothenburg Univ, Dept Clin Virol, S-41346 Gothenburg, Sweden

[2] Karolinska Inst, Div Clin Virol, Stockholm, Sweden

来源：

ANTIVIRAL RESEARCH | 2004年 / 61卷 / 02期

关键词：

glycyl-prolyl-glycine-amide; tripeptides; antiretroviral resistance;

D O I：

10.1016/j.antiviral.2003.09.003

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The chemically modified tripeptide glycyl-prolyl-glycine-amide (GPG-NH2) inhibits replication of HIV-1 in vitro, probably by interfering with capsid formation. This study was aimed at determining cross-resistance between antiretroviral drugs and GPG-NH2, and whether resistance to GPG-NH2 can be induced in vitro. Fifty-five clinical HIV-1 isolates with different resistance-related mutations were tested for susceptibility to GPG-NH2. No correlation between NRTI-, NNRTI- or PI-resistance and efficacy of GPG-NH2 was found, indicating the lack of cross-resistance. Serial passages were performed with GPG-NH2, and with lamivudine, and genotypic or phenotypic changes were determined. Resistance to lamivudine was detected after six passages. No resistance to GPG-NH2 was generated after 30 passages in two parallel series. However, one mutation (T 1071) in the p24 gene was detected in both series, but this mutation was not associated with decreased sensitivity to GPG-NH2. (C) 2003 Elsevier B.V. All rights reserved.

引用

页码：119 / 124

页数：6

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