scholarly journals DNA Triplex-Based Complexes Display Anti-HIV-1-Cell Fusion Activity

2015 ◽  
Vol 25 (4) ◽  
pp. 219-225 ◽  
Author(s):  
Liang Xu ◽  
Tao Zhang ◽  
Xiaoyu Xu ◽  
Huihui Chong ◽  
Wenqing Lai ◽  
...  
2021 ◽  
Vol 19 ◽  
Author(s):  
Liang Xu ◽  
Zeye Han ◽  
Hongqian Ren

Background: Human immunodeficiency virus type-1 (HIV-1) infection is the reason for the epidemic of acquired immunodeficiency syndrome (AIDS). Developing HIV-1 fusion inhibitors gained increasing attention as they took effect in the early stage of HIV-1 infecting cells. DNA G-quadruplex-based inhibitors had been found to interact with HIV-1 envelope glycoprotein, showing anti–HIV-1 fusion activity. C-peptide derived molecules with Met-Thr terminal also showed potent anti-fusion activity, the Met-Thr dipeptide adopted a hook-like structure (termed MT hook) in the hydrophobic pocket to "anchor" inhibitors to the N-terminal heptad repeat (NHR) of HIV-1 envelope glycoprotein gp41. Objective: Our work was to conjugate MT hooks to the 5'-terminal ends of DNA quadruplex-based inhibitor and demonstrate its biophysical characterization and anti–HIV-1 fusion activity. Methods: A 6-aminohexanol phosphonamidite was utilized in solid synthesis for the conjunction of oligodeoxynucleotide and MT dipeptide. Hydrophobic groups were introduced by a nucleoside analogue from the base site. Circular dichroism spectrum and native polyacrylamide gel electrophoresis were used to confirm the helix formation. A cell-cell fusion assay was carried out to test the anti-fusion activity. Results: The conjugate G1 showed improved anti-cell-cell fusion activity than quadruplex without MT hook. The MT hook did not affect the oligodeoxynucleotide (ODN) G-quadruplex assembly. It was also proved that G1 could effectively interfere with endogenous 6-helical bundle (6HB) formation between the N-terminal heptad repeat N36 (NHR) and the C-terminal heptad repeat C34 (CHR) during virus fusion course. Conclusion: In this work, conjugate of DNA-oligopeptide were successfully synthesized. The conjugation of MT hook did improve the anti-fusion activity of DNA G-quadruplex-based inhibitors. Our results can add information regarding on structure-activity relationships of DNA helix-based inhibitors and provide a reference for the follow-up experimental studies.


2018 ◽  
Vol 125 ◽  
pp. 244-253
Author(s):  
Yongjia Tang ◽  
Zeye Han ◽  
Hongqian Ren ◽  
Jiamei Guo ◽  
Huihui Chong ◽  
...  
Keyword(s):  
Anti Hiv ◽  
Hiv 1 ◽  

2019 ◽  
Vol 108 (7) ◽  
pp. 2243-2246 ◽  
Author(s):  
Zeye Han ◽  
Yongjia Tang ◽  
Hongqian Ren ◽  
Keliang Liu ◽  
Liang Xu

2018 ◽  
Vol 114 (3) ◽  
pp. 603a-604a
Author(s):  
Nejat Duzgunes ◽  
Michael Yee ◽  
Deborah Chau
Keyword(s):  
Anti Hiv ◽  
Hiv 1 ◽  

1989 ◽  
Vol 61 (01) ◽  
pp. 081-085 ◽  
Author(s):  
Simon Panzer ◽  
Christoph Stain ◽  
Hubert Hartl ◽  
Robert Dudczak ◽  
Klaus Lechner

SummaryLevels of anticardiolipin antibodies (ACA) were measured in 55 patients with haemophilia A in serum samples obtained in 1983 and in 1987. Twenty-one patients were negative for anti HIV-1 antibodies in 1983 and remained negative in 1987; 34 patients had anti HIV-1 antibodies in 1983; 17 of these latter patients remained asymptomatic, whereas 17 patients developed ARC or AIDS during the 4 years follow-up. Thirteen anti HIV-1 negative patients had elevated ACA levels in 1983; subsequently, a significant decrease was observed in all these subjects (p <0.001). All anti HIV-1 positive patients had elevated ACA levels in 1983; normal values were found in 9 patients in 1987. Yet, these changes were not significant (p >0.05). ACA levels were significantly higher in HIV-1 infected patients than in those without anti HIV-1 antibodies (p <0.05). There was no difference of ACA levels between the two anti HIV-1 positive patient groups, be it in 1983 or be it in 1987 (p >0.05). There was no correlation of ACA levels with serum IgG concentrations, CD4+ lymphocytes, or the consumption of factor VIII concentrates.


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