Gag Protein Oriented Supramolecular Nets as Potential HIV Traps

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-...

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Bibliographic Details
Published in:Bioconjugate chemistry 2021-01, Vol.32 (1), p.106-110
Main Authors: Zhou, Xi-Rui, Liu, Ye, Huang, Zhentao, Yao, Qingxin, He, Fangfei, Gao, Yuan
Format: Article
Language:English
Subjects:
Acquired immune deficiency syndrome
AIDS
Assembling
Conjugation
Drug development
Drug resistance
Gag protein
HIV
Human immunodeficiency virus
Nanofibers
Oxidation
Precursors
Proteins
Toxicity
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Summary: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.
ISSN:1043-1802
1520-4812
DOI:10.1021/acs.bioconjchem.0c00706