Anti HIV-1 effects

Moreover, antibody induction activities in mice were assayed for peptide tetramers 52c containing four peptide units, which were models of extracellular domains of an HIV-1 co-receptor CXR4, bound to la by click reaction with azides each containing two peptide units [141]. As a results, the linear peptide tetramers exhibited stronger antigenicity compared to the cyclic peptide mimics. Moreover, the anti-HIV-1 effects of induced antisera were assessed to reveal that linear peptide-induced antisera inhibited the HIV-1 entry significantly. 

CarbocycHc 2/3 -didehydro-2/3 -dideoxyguanosine [118353-05-2] (carbovk, CBV, 66), C H 2N502, synthesized in 1988 (177), is a promising candidate for the chemotherapy of AIDS. CBV inhibits HIV repHcation and HIV-induced cytopathic effects in a variety of human T-lymphoblastoid ceU lines at concentrations approximately two hundred- to four hundredfold below its cytotoxic concentrations (177). CBV is as effective as AZT and DDC in reducing the expression of vkal antigen in HIV-infected CEM ceUs (177). The antivkal potency and selectivity of carbovk is comparable to the anti-HIV-1 potency and selectivity of 2/3 -dideoxyadenosine (178). The exact mode of antivkal action of carbovk has not yet been elucidated, but may be the modulating effect of intraceUular nucleotides on 5 -nucleotidase activity (179). 

IhRNAs have also been used to induce an anti-HIV-1 RNAi response (Barichievy et al. 2007 Konstantinova et al. 2006, 2007 Liu et al. 2007). These IhRNAs can be processed into multiple effective siRNAs, thus preventing the chance of viral escape. Although IhRNA have been shown to effectively inhibit HIV-1 replication, there is currently no data on their ability to prevent viral escape. The use of multiple siRNAs or IhRNAs should take into account the increased danger of side effects due to interference with cellular miRNA processing and function. 

A study of anti-HIV replication effects of nearly 50 imino sugars demonstrated that A-alkyl derivatives of 1-deoxynojirimycin exhibit markedly enhanced activity when compared to the unsubstituted parent compound. In particular, compound 131... 

Avarol and avarone derivatives (from the Red Sea sponge Dysidea cinerea), the alkaloids psy-chotrine and O-methylpsychotrine (from ipecac, the dried rhizome and root of Cephaelis ipecacuanha), and phloroglucinol derivatives such as mallotojaponin, from the pericarps of Mallotus japonicus, have all been reported to inhibit the reverse transcriptase activity of HIV-1, noncom-petitively with respect to the natural substrate (dNTP). In neither case was the anti-HIV-1 activity determined in cell culture, so it is not clear whether any of these compounds is really an effective... 

Anti-HIV-1 Activity of Calanolides in Hollow Fiber Mouse Evaluation of (-l-)-calanolide A (1) in a hollow fiber culture-based in a SCID mouse assay of antiviral efficacy indicated that (+)-calanolide A exhibited significant anti-HIV-1 activity after oral or parenteral administration on a once-daily (200mg/kg/ dose) or twice-daily (150 mg/kg/dose) treatment. Furthermore, a synergistic effect was observed in the combination of (-l-)-calanolide A and AZT. ... 

Another study also investigated the effect of various anti-Rev aptamers in vivo, but from a somewhat different angle. Symensma et al. substituted the wild-type Rev-binding element for the Rev-binding aptamer, and tested whether the synthetic Rev-binding RNA would still be able to substitute the biological function of the wild-type, i.e.Ao facilitate Rev-dependent mRNA transport [72]. Various classes of anti-HIV-1-Rev-binding aptamers were assayed One class closely resembled the wild-type sequence, whereas the... 

Izumi K, Watanabe K, Oishi S et al (2011) Potent anti-HIV-1 activity of N-HR-derived peptides including a deep pocket-forming region without antagonistic effects on T-20. Antiviral Chem Chemother 22 51-55... 

Hale, f.f.et al. (2002) 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3 polar functionality and its effect on anti-HIV-1 activity. Bioorgank ej Medicinal Chemistry Letters, 12 (20), 2997-3000. 

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