Gag Protein Oriented Supramolecular Nets as Potential HIV Traps,Bioconjugate Chemistry

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Gag Protein Oriented Supramolecular Nets as Potential HIV Traps
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2021-01-06 , DOI: 10.1021/acs.bioconjchem.0c00706
Xi-Rui Zhou ₁ , Ye Liu ₂ , Zhentao Huang ₃ , Qingxin Yao ₃ , Fangfei He ₃ , Yuan Gao ₃

Affiliation

For HIV/AIDS treatment, the cocktail therapy which uses a combination of anti-retroviral drugs remains the most widely accepted practice. However, the potential drug toxicity, patient tolerability, and emerging drug resistance have limited its long-term efficiency. Here, we design a HIV Gag protein-targeting redox supramolecular assembly (ROSA) system for potential HIV inhibition. An assembling precursor was constructed through conjugation of an oxidation-activatable fluorogenic compound BQA with a selected tetrapeptide GGFF. Since BQA shares a similar structure with the known Gag inhibitor, the precursor could bind to HIV Gag protein with moderate affinity. Moreover, after oxidation, the corresponding nanofibers could bind to Gag protein and trap HIV to realize virus control, thus providing a potential anti-HIV strategy.

中文翻译：

Gag 蛋白定向超分子网作为潜在的 HIV 陷阱

对于 HIV/AIDS 治疗，使用抗逆转录病毒药物组合的鸡尾酒疗法仍然是最广泛接受的做法。然而，潜在的药物毒性、患者耐受性和新出现的耐药性限制了其长期疗效。在这里，我们设计了一种 HIV Gag 蛋白靶向氧化还原超分子组装 (ROSA) 系统，用于潜在的 HIV 抑制。通过将可氧化激活的荧光化合物 BQA 与选定的四肽 GGFF 结合来构建组装前体。由于 BQA 与已知的 Gag 抑制剂具有相似的结构，因此前体可以以中等亲和力与 HIV Gag 蛋白结合。此外，氧化后相应的纳米纤维可以与Gag蛋白结合并捕获HIV以实现病毒控制，从而提供潜在的抗HIV策略。

更新日期：2021-01-20

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