ArticleJournal of molecular recognition : JMR
Introducing metallocene into a triazole peptide conjugate reduces its off-rate and enhances its affinity and antiviral potency for HIV-1 gp120.
Article in Journal of molecular recognition : JMR. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 45 citations in OpenAlex.
- A Literature Review Focusing on the Antiviral Activity of [1,2,4] and [1,2,3]-triazoles.Mini reviews in medicinal chemistry · 2024Review
- Peptide Triazole Inhibitors of HIV-1: Hijackers of Env Metastability.Current protein & peptide science · 2023Review
- Peptide-Based HIV Entry Inhibitors.Advances in experimental medicine and biology · 2022Article
- Impact of non-proteinogenic amino acids in the discovery and development of peptide therapeutics.Amino acids · 2020Review
- Chemical optimization of macrocyclic HIV-1 inactivators for improving potency and increasing the structural diversity at the triazole ring.Organic & biomolecular chemistry · 2017Article
- Impact of HIV-1 Membrane Cholesterol on Cell-Independent Lytic Inactivation and Cellular Infectivity.Biochemistry · 2016Article
- Short Communication: Inhibition of DC-SIGN-Mediated HIV-1 Infection by Complementary Actions of Dendritic Cell Receptor Antagonists and Env-Targeting Virus Inactivators.AIDS research and human retroviruses · 2016Article
- Macrocyclic Envelope Glycoprotein Antagonists that Irreversibly Inactivate HIV-1 before Host Cell Encounter.Journal of medicinal chemistry · 2015Article
- Peptide Triazole Inactivators of HIV-1 Utilize a Conserved Two-Cavity Binding Site at the Junction of the Inner and Outer Domains of Env gp120.Journal of medicinal chemistry · 2015Article
- Mechanism of multivalent nanoparticle encounter with HIV-1 for potency enhancement of peptide triazole virus inactivation.The Journal of biological chemistry · 2015Article
- Peptide triazole inactivators of HIV-1: how do they work and what is their potential?Future medicinal chemistry · 2015Article
- Covalent conjugation of a peptide triazole to HIV-1 gp120 enables intramolecular binding site occupancy.Biochemistry · 2014Article
- Synthesis and antioxidant evaluation of enantiomerically pure bis-(1,2,3-triazolylmethyl)amino esters from modified α-amino acids.TheScientificWorldJournal · 2014Article
- Interactions of peptide triazole thiols with Env gp120 induce irreversible breakdown and inactivation of HIV-1 virions.Retrovirology · 2013Article
- Click chemistry in peptide-based drug design.Molecules (Basel, Switzerland) · 2013Review
- A model of peptide triazole entry inhibitor binding to HIV-1 gp120 and the mechanism of bridging sheet disruption.Biochemistry · 2013Article
- Non-natural peptide triazole antagonists of HIV-1 envelope gp120.ChemMedChem · 2013Article
- HIV-1 Env gp120 structural determinants for peptide triazole dual receptor site antagonism.Proteins · 2013Article
- Antiviral breadth and combination potential of peptide triazole HIV-1 entry inhibitors.Antimicrobial agents and chemotherapy · 2012Article
- Cell-free HIV-1 virucidal action by modified peptide triazole inhibitors of Env gp120.ChemMedChem · 2011Article
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Authors and funding
11 authors at 2 institutions in 1 country.
Funding
Abstract
In this work, we identified a high affinity and potency metallocene-containing triazole peptide conjugate that suppresses the interactions of HIV-1 envelope gp120 at both its CD4 and co-receptor binding sites. The ferrocene-peptide conjugate, HNG-156, was formed by an on-resin copper-catalysed [2+3] cycloaddition reaction. Surface plasmon resonance interaction analysis revealed that, compared to a previously reported phenyl-containing triazole conjugate HNG-105 (105), peptide 156 had a higher direct binding affinity for several subtypes of HIV-1 gp120 due mainly to the decreased dissociation rate of the conjugate-gp120 complex. The ferrocene triazole conjugate bound to gp120 of both clade A (92UG037-08) and clade B (YU-2 and SF162) virus subtypes with nanomolar KD in direct binding and inhibited the binding of gp120 to soluble CD4 and to antibodies that bind to HIV-1YU-2 gp120 at both the CD4 binding site and CD4-induced binding sites. HNG-156 showed a close-to nanomolar IC50 for inhibiting cell infection by HIV-1BaL whole virus. The dual receptor site antagonist activity and potency of HNG-156 make it a promising viral envelope inhibitor lead for developing anti-HIV-1 treatments.
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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.