ArticleBioconjugate chemistry2012
Design of a modular tetrameric scaffold for the synthesis of membrane-localized D-peptide inhibitors of HIV-1 entry.
Article in Bioconjugate chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed.
- The SMARCA4-TMEM47 axis plays an essential role in chikungunya virus RNA replication.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- Electron tomography visualization of HIV-1 virions trapped by fusion inhibitors to host cells in infected tissues.Journal of virology · 2024Article
- Article
- Prevention and treatment of SHIVAD8 infection in rhesus macaques by a potent d-peptide HIV entry inhibitor.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- Characterization of resistance to a potent D-peptide HIV entry inhibitor.Retrovirology · 2019Article
- Pharmacokinetic and Chemical Synthesis Optimization of a Potent d-Peptide HIV Entry Inhibitor Suitable for Extended-Release Delivery.Molecular pharmaceutics · 2018Article
- Aligator: A computational tool for optimizing total chemical synthesis of large proteins.Bioorganic & medicinal chemistry · 2017Review
- Inhibition of HIV Entry by Targeting the Envelope Transmembrane Subunit gp41.Current HIV research · 2016Review
- Cholesterol-conjugated peptide antivirals: a path to a rapid response to emerging viral diseases.Journal of peptide science : an official publication of the European Peptide Society · 2015Review
- Design and characterization of ebolavirus GP prehairpin intermediate mimics as drug targets.Protein science : a publication of the Protein Society · 2015Article
- Dramatic potentiation of the antiviral activity of HIV antibodies by cholesterol conjugation.The Journal of biological chemistry · 2014Article
- Multivalent antiviral XTEN-peptide conjugates with long in vivo half-life and enhanced solubility.Bioconjugate chemistry · 2014Article
- Fatal measles virus infection prevented by brain-penetrant fusion inhibitors.Journal of virology · 2013Article
- Modular assembly of dimeric HIV fusion inhibitor peptides with enhanced antiviral potency.Bioorganic & medicinal chemistry letters · 2013Article
- Novel preclinical models of topical PrEP pharmacodynamics provide rationale for combination of drugs with complementary properties.Retrovirology · 2013Article
- Single molecular weight discrete PEG compounds: emerging roles in molecular diagnostics, imaging and therapeutics.Expert review of molecular diagnostics · 2013Article
- Non-natural peptide triazole antagonists of HIV-1 envelope gp120.ChemMedChem · 2013Article
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4 authors.
Funding
Abstract
The highly conserved HIV-1 gp41 "pocket" region is a promising target for inhibiting viral entry. PIE12-trimer is a protease-resistant trimeric d-peptide inhibitor that binds to this pocket and potently blocks HIV entry. PIE12-trimer also possesses a reserve of binding energy that provides it with a strong genetic barrier to resistance ("resistance capacitor"). Here, we report the design of a modular scaffold employing PEGs of discrete lengths for the efficient optimization and synthesis of PIE12-trimer. This scaffold also allows us to conjugate PIE12-trimer to several membrane-localizing cargoes, resulting in dramatically improved potency and retention of PIE12-trimer's ability to absorb the impact of resistance mutations. This scaffold design strategy should be of broad utility for the rapid prototyping of multimeric peptide inhibitors attached to potency- or pharmacokinetics-enhancing groups.
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