ArticleNature chemical biology2014
A broad HIV-1 inhibitor blocks envelope glycoprotein transitions critical for entry.
Article in Nature chemical biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 59 papers, 1 of them a synthesis that pooled it.
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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
59 citing papers in PubMed, 1 synthesis or guideline pooled it, 84 citations in OpenAlex.
- HIV Genome-Wide Protein Associations: a Review of 30 Years of Research.Microbiology and molecular biology reviews : MMBR · 2016Pooled it
- Fostemsavir Decreases the Levels of Anti-gp120 CD4-Induced Antibodies in Heavily Treatment-Experienced People With HIV.The Journal of infectious diseases · 2026Article
- Highly efficient production of HIV-1Journal of virology · 2025Article
- Evaluating the Immune Response in Rabbits to an Escalating Dose of mRNA-Based HIV-1 Env Immunogens.Vaccines · 2025Article
- Incompletely closed HIV-1Npj viruses · 2025Article
- mRNA-based HIV-1 vaccines.Clinical microbiology reviews · 2024Review
- Conformational flexibility of HIV-1 envelope glycoproteins modulates transmitted/founder sensitivity to broadly neutralizing antibodies.Nature communications · 2024Article
- A Narrative Review of the State of the Art of CCR4-Based Therapies in Cutaneous T-Cell Lymphomas: Focus on Mogamulizumab and Future Treatments.Antibodies (Basel, Switzerland) · 2024Review
- Alternative substitutions of N332 in HIV-1mBio · 2024Article
- HIResist: a database of HIV-1 resistance to broadly neutralizing antibodies.Bioinformatics (Oxford, England) · 2024Article
- Article
- Conformational flexibility of HIV-1 envelope glycoproteins modulates transmitted / founder sensitivity to broadly neutralizing antibodies.bioRxiv : the preprint server for biology · 2023Article
- V3 tip determinants of susceptibility to inhibition by CD4-mimetic compounds in natural clade A human immunodeficiency virus (HIV-1) envelope glycoproteins.Journal of virology · 2023Article
- Enhancing anti-viral neutralization response to immunization with HIV-1 envelope glycoprotein immunogens.NPJ vaccines · 2023Article
- Alternative substitutions of N332 in HIV-1bioRxiv : the preprint server for biology · 2023Article
- Structure-function analyses reveal key molecular determinants of HIV-1 CRF01_AE resistance to the entry inhibitor temsavir.Nature communications · 2023Article
- Isomerization of bioactive acylhydrazones triggered by light or thiols.Nature chemistry · 2023Article
- Temsavir blocks the immunomodulatory activities of HIV-1 soluble gp120.Cell chemical biology · 2023Article
- Acylhydrazones and Their Biological Activity: A Review.Molecules (Basel, Switzerland) · 2022Review
- Broad Tricyclic Ring Inhibitors Block SARS-CoV-2 Spike Function Required for Viral Entry.ACS infectious diseases · 2022Article
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
Abstract
Binding to the primary receptor, CD4, triggers conformational changes in the metastable HIV-1 envelope glycoprotein (Env) trimer ((gp120-gp41)3) that are important for virus entry into host cells. These changes include an 'opening' of the trimer, creation of a binding site for the CCR5 co-receptor and formation and/or exposure of a gp41 coiled coil. Here we identify a new compound, 18A (1), that specifically inhibits the entry of a wide range of HIV-1 isolates. 18A does not interfere with CD4 or CCR5 binding, but it inhibits the CD4-induced disruption of quaternary structures at the trimer apex and the exposure of the gp41 HR1 coiled coil. Analysis of HIV-1 variants with increased or reduced sensitivity to 18A suggests that the inhibitor can distinguish distinct conformational states of gp120 in the unliganded Env trimer. The broad-range activity and observed hypersensitivity of resistant mutants to antibody neutralization support further investigation of 18A.
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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.