The Australian Institute for Bioengineering and Nanotechnology, The University of Queensland, St Lucia, QLD, 4072, Australia.
The School of Chemistry and Molecular Biosciences, The University of Queensland, St Lucia, QLD, 4072, Australia.
Virol J. 2024 Jan 10;21(1):14. doi: 10.1186/s12985-024-02288-z.
The human T-lymphotropic virus type 1 (HTLV-1) infects millions of people globally and is endemic to various resource-limited regions. Infections persist for life and are associated with increased susceptibility to opportunistic infections and severe diseases including adult T cell leukemia/lymphoma and HTLV-1-associated myelopathy-tropical spastic paraparesis. No HTLV-1-specific anti-retrovirals have been developed and it is unclear whether existing anti-retrovirals developed for treatment of human immunodeficiency virus (HIV) have efficacy against HTLV-1. To understand the structural basis for therapeutic binding, homology modelling and machine learning were used to develop a structural model of the HTLV-1 reverse transcriptase. With this, molecular docking experiments using a panel of FDA-approved inhibitors of viral reverse transcriptases to assess their capacity for binding, and in turn, inhibition. Importantly, nucleoside/nucleotide reverse transcriptase inhibitor but not non-nucleoside reverse transcriptase inhibitors were predicted to bind the HTLV-1 reverse transcriptase, with similar affinity to HIV-1 reverse transcriptase. By strengthening the rationale for clinical testing of therapies such as tenofovir alafenamide, zidovudine, lamivudine, and azvudine for treatment of HTLV-1, this study has demonstrated the power of in silico structural biology approaches in drug design and therapeutic testing.
人类 T 淋巴细胞白血病病毒 1 型(HTLV-1)在全球感染了数百万人,在各种资源有限的地区流行。感染会持续终生,并与机会性感染和严重疾病的易感性增加有关,包括成人 T 细胞白血病/淋巴瘤和 HTLV-1 相关脊髓病-热带痉挛性截瘫。目前尚未开发出针对 HTLV-1 的抗逆转录病毒药物,也不清楚现有的用于治疗人类免疫缺陷病毒(HIV)的抗逆转录病毒药物是否对 HTLV-1 有效。为了了解治疗结合的结构基础,使用同源建模和机器学习开发了 HTLV-1 逆转录酶的结构模型。利用该模型,通过分子对接实验使用一组 FDA 批准的病毒逆转录酶抑制剂来评估它们的结合能力,进而评估抑制能力。重要的是,预测核苷/核苷酸逆转录酶抑制剂而非非核苷逆转录酶抑制剂与 HTLV-1 逆转录酶结合,与 HIV-1 逆转录酶的亲和力相似。通过加强替诺福韦艾拉酚胺、齐多夫定、拉米夫定和阿扎那韦等治疗方法的临床测试的理由,本研究证明了计算结构生物学方法在药物设计和治疗测试中的强大功能。