ArticleAntimicrobial agents and chemotherapy2008
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
Article in Antimicrobial agents and chemotherapy, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 39 citations in OpenAlex.
- Polyether antibiotics K-41A and K-41Am inhibit HIV-1 replication via suppressing the activities of HIV-1 reverse transcriptase and integrase.Archives of medical science : AMS · 2025Article
- The Use of Zidovudine Pharmacophore in Multi-Target-Directed Ligands for AIDS Therapy.Molecules (Basel, Switzerland) · 2022Review
- The Genesis and Future Prospects of Small Molecule HIV-1 Attachment Inhibitors.Advances in experimental medicine and biology · 2022Review
- Coronil, a Tri-Herbal Formulation, Attenuates Spike-Protein-Mediated SARS-CoV-2 Viral Entry into Human Alveolar Epithelial Cells and Pro-Inflammatory Cytokines Production by Inhibiting Spike Protein-ACE-2 Interaction.Journal of inflammation research · 2021Article
- Design and Synthesis of Quinolizidine Derivatives as Influenza Virus and HIV-1 Inhibitors.Current medicinal chemistry · 2021Article
- Novel Betulinic Acid-Nucleoside Hybrids with Potent Anti-HIV Activity.ACS medicinal chemistry letters · 2020Article
- Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities.European journal of medicinal chemistry · 2020Article
- Structure and Anti-HIV Activity of Betulinic Acid Analogues.Current medical science · 2018Review
- Structure Optimization of Aloperine Derivatives as HIV-1 Entry Inhibitors.ACS medicinal chemistry letters · 2017Article
- Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1.Journal of medicinal chemistry · 2016Article
- Identification and Characterization of BMS-955176, a Second-Generation HIV-1 Maturation Inhibitor with Improved Potency, Antiviral Spectrum, and Gag Polymorphic Coverage.Antimicrobial agents and chemotherapy · 2016Article
- Aloperine and Its Derivatives as a New Class of HIV-1 Entry Inhibitors.ACS medicinal chemistry letters · 2016Article
- New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1.Journal of medicinal chemistry · 2013Article
- Review
- Synthesis of betulinic acid derivatives as entry inhibitors against HIV-1 and bevirimat-resistant HIV-1 variants.Bioorganic & medicinal chemistry letters · 2012Article
- The role of dynamin in HIV type 1 Env-mediated cell-cell fusion.AIDS research and human retroviruses · 2011Article
- HIV envelope: challenges and opportunities for development of entry inhibitors.Trends in microbiology · 2011Review
- A low-molecular-weight entry inhibitor of both CCR5- and CXCR4-tropic strains of human immunodeficiency virus type 1 targets a novel site on gp41.Journal of virology · 2010Article
- Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors.Journal of medicinal chemistry · 2009Article
- Plant-derived triterpenoids and analogues as antitumor and anti-HIV agents.Natural product reports · 2009Review
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
Abstract
Betulinic acid (BA) derivatives can inhibit human immunodeficiency virus type 1 (HIV-1) entry or maturation depending on side chain modifications. While BA derivatives with antimaturation activity have attracted considerable interest, the anti-HIV-1 profile and molecular mechanism of BA derivatives with anti-HIV-1 entry activity (termed BA entry inhibitors) have not been well defined. In this study, we have found that two BA entry inhibitors, IC9564 and A43D, exhibited a broad spectrum of anti-HIV-1 activity. Both compounds inhibited multiple strains of HIV-1 from clades A, B, and C at submicromolar concentrations. Clade C viruses were more sensitive to the compounds than clade A and B viruses. Interestingly, IC9564 at subinhibitory concentrations could alter the antifusion activities of other entry inhibitors. IC9564 was especially potent in increasing the sensitivity of HIV-1 YU2 Env-mediated membrane fusion to the CCR5 inhibitor TAK-779. Results from this study suggest that the V3 loop of gp120 is a critical determinant for the anti-HIV-1 activity of IC9564. IC9564 escape viruses contained mutations near the tip of the V3 loop. Moreover, IC9564 could compete with the binding of V3 monoclonal antibodies 447-52D and 39F. IC9564 also competed with the binding of gp120/CD4 complexes to chemokine receptors. In summary, these results suggest that BA entry inhibitors can potently inhibit a broad spectrum of primary HIV-1 isolates by targeting the V3 loop of gp120.
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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.