Larder B A, Chesebro B, Richman D D
Department of Molecular Sciences, Wellcome Research Laboratories, Beckenham, Kent, United Kingdom.
Antimicrob Agents Chemother. 1990 Mar;34(3):436-41. doi: 10.1128/AAC.34.3.436.
Conventional assays based on infection of T-cell lymphoblastoid lines with tissue culture-adapted strains of human immunodeficiency virus (HIV) are well established and have been used successfully to discover potent inhibitors of HIV replication. In this report we show that such assays are not easily applied to testing the susceptibilities of clinical HIV isolates to inhibitors because of differences in replication rates and cytotoxicity, thus demonstrating that conventional HIV assays should be used with caution when the zidovudine susceptibility of clinical isolates is assessed. An assay based on plaque reduction in CD4+ HeLa cell monolayers was validated by determining susceptibilities of HIV to a large number of inhibitors in this system. In general, 50% inhibitory doses for HIV type 1 and 2 strains derived from plaque reduction data were in good agreement with susceptibility data obtained by using conventional assays with T-cell lines. The susceptibilities of previously identified zidovudine-resistant HIV isolates to a large group of inhibitors, including nonucleosides, such as interferons and soluble CD4, were tested by using a plaque reduction assay in CD4+ HeLa cells. Surprisingly, an extremely narrow range of cross resistance was observed; cross resistance was limited to nucleoside analogs containing a 3'-azido group. These data point the way to the use of combinations of inhibitors to delay the appearance of drug resistance.
基于用人免疫缺陷病毒(HIV)的组织培养适应株感染T细胞淋巴母细胞系的传统检测方法已经确立,并已成功用于发现HIV复制的有效抑制剂。在本报告中,我们表明,由于复制速率和细胞毒性的差异,此类检测方法不易应用于检测临床HIV分离株对抑制剂的敏感性,因此表明在评估临床分离株的齐多夫定敏感性时,应谨慎使用传统的HIV检测方法。通过测定该系统中HIV对大量抑制剂的敏感性,验证了基于CD4+HeLa细胞单层蚀斑减少的检测方法。一般来说,从蚀斑减少数据得出的1型和2型HIV毒株的50%抑制剂量与使用T细胞系的传统检测方法获得的敏感性数据高度一致。通过在CD4+HeLa细胞中进行蚀斑减少检测,测试了先前鉴定的齐多夫定耐药HIV分离株对一大类抑制剂的敏感性,这些抑制剂包括非核苷类,如干扰素和可溶性CD4。令人惊讶的是,观察到的交叉耐药范围极窄;交叉耐药仅限于含有3'-叠氮基的核苷类似物。这些数据为使用抑制剂组合来延缓耐药性的出现指明了方向。