ArticleMolecules (Basel, Switzerland)2018
Kinetic Characterization of Novel HIV-1 Entry Inhibitors: Discovery of a Relationship between Off-Rate and Potency.
Article in Molecules (Basel, Switzerland), 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- Design, synthesis, and mechanistic study of 2-piperazineone-bearing peptidomimetics as novel HIV capsid modulators.RSC medicinal chemistry · 2023Article
- Structure-Based Identification of Natural-Product-Derived Compounds with Potential to Inhibit HIV-1 Entry.Molecules (Basel, Switzerland) · 2023Article
- Identification of human immunodeficiency virus -1 E protein-targeting lead compounds by pharmacophore based screening.Saudi medical journal · 2022Article
- Design, synthesis, and mechanism study of dimerized phenylalanine derivatives as novel HIV-1 capsid inhibitors.European journal of medicinal chemistry · 2021Article
- Rapid Optimization of the Metabolic Stability of a Human Immunodeficiency Virus Type-1 Capsid Inhibitor Using a Multistep Computational Workflow.Journal of medicinal chemistry · 2021Article
- Field-Based Affinity Optimization of a Novel Azabicyclohexane Scaffold HIV-1 Entry Inhibitor.Molecules (Basel, Switzerland) · 2019Article
- Controllable Preparation of SERS-Active Ag-FeS Substrates by a Cosputtering Technique.Molecules (Basel, Switzerland) · 2019Article
- Discovery of phenylalanine derivatives as potent HIV-1 capsid inhibitors from click chemistry-based compound library.European journal of medicinal chemistry · 2018Article
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Authors and funding
4 authors.
Funding
Abstract
The entry of HIV-1 into permissible cells remains an extremely attractive and underexploited therapeutic intervention point. We have previously demonstrated the ability to extend the chemotypes available for optimization in the entry inhibitor class using computational means. Here, we continue this effort, designing and testing three novel compounds with the ability to inhibit HIV-1 entry. We demonstrate that alteration of the core moiety of these entry inhibitors directly influences the potency of the compounds, despite common proximal and distal groups. Moreover, by establishing for the first time a surface plasmon resonance (SPR)-based interaction assay with soluble recombinant SOSIP Env trimers, we demonstrate that the off-rate (k
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