Institute of Virology, Medical Faculty, Heinrich Heine University Düsseldorf, 40225 Düsseldorf, Germany.
Int J Mol Sci. 2021 Dec 23;23(1):156. doi: 10.3390/ijms23010156.
The underlying molecular mechanism and their general effect on the replication capacity of HIV 1 drug-resistance-associated mutations is often poorly understood. To elucidate the effect of two such mutations located in a region with a high density of spicing regulatory elements on the HIV-1-splicing outcome, bioinformatic predictions were combined with transfection and infection experiments. Results show that the previously described R263K drug-resistance-associated integrase mutation has additionally a severe effect on the ESE2b splicing regulatory element (SRE) in exon 2b, which causes loss of SD2b recognition. This was confirmed by an R263R silent mutation with a similar predicted effect on the exon 2b SRE. In contrast, a V260I mutation and its silent counterpart with a lower effect on ESS2b did not exhibit any differences in the splicing pattern. Since HIV-1 highly relies on a balanced splicing reaction, changes in the splicing outcome can contribute to changes in viral replication and might add to the effect of escape mutations toward antiviral drugs. Thus, a classification of mutations purely addressing proteins is insufficient.
这些耐药相关突变的潜在分子机制及其对 HIV-1 复制能力的普遍影响往往了解甚少。为了阐明位于剪接调控元件高度密集区的两个突变对 HIV-1 剪接结果的影响,我们将生物信息学预测与转染和感染实验相结合。结果表明,先前描述的 R263K 耐药相关整合酶突变对 2b 外显子中的 ESE2b 剪接调控元件(SRE)具有严重影响,导致 SD2b 识别丧失。这通过具有相似预测对 2b 外显子 SRE 作用的 R263R 沉默突变得到证实。相比之下,V260I 突变及其对 ESS2b 影响较低的沉默对应物在剪接模式上没有差异。由于 HIV-1 高度依赖于平衡的剪接反应,剪接结果的变化可能导致病毒复制的变化,并可能增加对抗病毒药物的逃逸突变的影响。因此,纯粹针对蛋白质的突变分类是不够的。