Kitchen Christina M R, Krogstad Paul, Kitchen Scott G
Department of Biostatistics, UCLA School of Public Health, Los Angeles, California 90095, USA.
Open Med Inform J. 2010;4:225-32. doi: 10.2174/1874431101004010225. Epub 2010 Dec 3.
Although antiretroviral drug resistance is common in treated HIV infected individuals, it is not a consistent indicator of HIV morbidity and mortality. To the contrary, HIV resistance-associated mutations may lead to changes in viral fitness that are beneficial to infected individuals. Using a bioinformatics-based model to assess the effects of numerous drug resistance mutations, we determined that the D30N mutation in HIV-1 protease had the largest decrease in replication capacity among known protease resistance mutations. To test this in silico result in an in vivo environment, we constructed several drug-resistant mutant HIV-1 strains and compared their relative fitness utilizing the SCID-hu mouse model. We found HIV-1 containing the D30N mutation had a significant defect in vivo, showing impaired replication kinetics and a decreased ability to deplete CD4+ thymocytes, compared to the wild-type or virus without the D30N mutation. In comparison, virus containing the M184V mutation in reverse transcriptase, which shows decreased replication capacity in vitro, did not have an effect on viral fitness in vivo. Thus, in this study we have verified an in silico bioinformatics result with a biological assessment to identify a unique mutation in HIV-1 that has a significant fitness defect in vivo.
尽管抗逆转录病毒药物耐药性在接受治疗的HIV感染者中很常见,但它并非HIV发病和死亡的一致指标。相反,与HIV耐药相关的突变可能导致病毒适应性的变化,这对感染者有益。使用基于生物信息学的模型来评估众多耐药突变的影响,我们确定HIV-1蛋白酶中的D30N突变在已知的蛋白酶耐药突变中复制能力下降幅度最大。为了在体内环境中验证这一计算机模拟结果,我们构建了几种耐药突变型HIV-1毒株,并利用SCID-hu小鼠模型比较它们的相对适应性。我们发现,与野生型或不含D30N突变的病毒相比,含有D30N突变的HIV-1在体内存在显著缺陷,表现为复制动力学受损以及耗尽CD4+胸腺细胞的能力下降。相比之下,在体外显示复制能力下降的逆转录酶中含有M184V突变的病毒,在体内对病毒适应性没有影响。因此,在本研究中,我们通过生物学评估验证了计算机模拟生物信息学结果,以确定HIV-1中一个在体内具有显著适应性缺陷的独特突变。