ArticleBiomacromolecules2012
Polyvalent side chain peptide-synthetic polymer conjugates as HIV-1 entry inhibitors.
Article in Biomacromolecules, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
9 citing papers in PubMed, 49 citations in OpenAlex.
- Polymer Conjugate as the New Promising Drug Delivery System for Combination Therapy against Cancer.Current topics in medicinal chemistry · 2024Review
- Biomolecular Densely Grafted Brush Polymers: Oligonucleotides, Oligosaccharides and Oligopeptides.Angewandte Chemie (International ed. in English) · 2020Review
- Site-Specific Polymer Attachment to HR2 Peptide Fusion Inhibitors against HIV-1 Decreases Binding Association Rates and Dissociation Rates Rather Than Binding Affinity.Bioconjugate chemistry · 2017Article
- Mechanisms of fast and stringent search in homologous pairing of double-stranded DNA.PLoS computational biology · 2017Article
- Responsive Hybrid (Poly)peptide-Polymer Conjugates.Journal of materials chemistry. B · 2017Article
- Designing multivalent probes for tunable superselective targeting.Proceedings of the National Academy of Sciences of the United States of America · 2015Article
- Recent advances in engineering polyvalent biological interactions.Biomacromolecules · 2015Review
- Optimizing the Selectivity of Surface-Adsorbing Multivalent Polymers.Macromolecules · 2014Article
- Superselective targeting using multivalent polymers.Journal of the American Chemical Society · 2014Article
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 2 countries.
Funding
Abstract
This report describes the synthesis and properties of a series of polyvalent side chain peptide-synthetic polymer conjugates designed to block the CD4 binding site on gp120 and inhibit HIV-1 entry into a host cell. The peptide sequences in the conjugates are based on the CDR H3 region of the neutralizing anti-HIV-1 antibody IgG1 b12. Using a consecutive ester-amide/thiol-ene postpolymerization modification strategy, a library of polymer conjugates was prepared. Evaluation of the HIV-1 inhibitory properties revealed that midsized polymer conjugates displayed the highest antiviral activity, while shorter and longer conjugates proved to be less efficacious inhibitors. The lower molecular weight conjugates may not have sufficient length to span the distance between two neighboring gp120 containing spikes, while the higher molecular weight conjugates may be compromised due to a higher entropic penalty that would accompany their binding to the viral envelope. Although the IC(50) values for these polymer conjugates are higher than that of the parent IgG1 b12 antibody, the strategy presented here may represent an interesting antiviral approach due to the attractive properties of such polymer therapeutics (relatively inexpensive production and purification costs, high thermal and chemical stability in storage conditions, long half-life in biological tissues, low immunogenicity, and protection from proteolytic degradation).
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.