ArticleAntimicrobial agents and chemotherapy2012
Preclinical evaluation of the HIV-1 fusion inhibitor L'644 as a potential candidate microbicide.
Article in Antimicrobial agents and chemotherapy, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed.
- Antiviral Activity and Mucosal Safety of Novel Human-Milk-Inspired Antimicrobial Peptides.Pharmaceutics · 2026Article
- Nanobody-Based Bioconjugates as Potent and Broadly Active Inhibitors of HIV Entry.Journal of the American Chemical Society · 2026Article
- Article
- Peptide Amphiphilic-Based Supramolecular Structures with Anti-HIV-1 Activity.Bioconjugate chemistry · 2021Article
- Article
- Importance of structure-based studies for the design of a novel HIV-1 inhibitor peptide.Scientific reports · 2020Article
- Lipid Vesicles Loaded with an HIV-1 Fusion Inhibitor Peptide as a Potential Microbicide.Pharmaceutics · 2020Article
- The Pre-clinical Toolbox of Pharmacokinetics and Pharmacodynamics:Frontiers in pharmacology · 2019Review
- Pharmaceutical Approaches to HIV Treatment and Prevention.Advanced therapeutics · 2018Article
- Development of peptide inhibitors of HIV transmission.Bioactive materials · 2016Review
- Human Immunodeficiency Virus Immune Cell Receptors, Coreceptors, and Cofactors: Implications for Prevention and Treatment.AIDS patient care and STDs · 2016Review
- Inhibition of HIV Entry by Targeting the Envelope Transmembrane Subunit gp41.Current HIV research · 2016Review
- Animal and human mucosal tissue models to study HIV biomedical interventions: can we predict success?Journal of the International AIDS Society · 2015Review
- Mapping antiretroviral drugs in tissue by IR-MALDESI MSI coupled to the Q Exactive and comparison with LC-MS/MS SRM assay.Journal of the American Society for Mass Spectrometry · 2014Article
- Improvement of HIV fusion inhibitor C34 efficacy by membrane anchoring and enhanced exposure.The Journal of antimicrobial chemotherapy · 2014Article
- Rectal microbicide development.Current topics in microbiology and immunology · 2014Review
- Rectal pre-exposure prophylaxis (PrEP).Antiviral research · 2013Review
- Use of human mucosal tissue to study HIV-1 pathogenesis and evaluate HIV-1 prevention modalities.Current HIV/AIDS reports · 2013Review
- Conjugation of cholesterol to HIV-1 fusion inhibitor C34 increases peptide-membrane interactions potentiating its action.PloS one · 2013Article
- Rectal microbicide development.Current opinion in HIV and AIDS · 2012Review
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
Topical blockade of the gp41 fusogenic protein of HIV-1 is one possible strategy by which microbicides could prevent HIV transmission, working early against infection, by inhibiting viral entry into host cells. In this study, we examined the potential of gp41 fusion inhibitors (FIs) as candidate anti-HIV microbicides. Preclinical evaluation of four FIs, C34, T20, T1249, and L'644, was performed using cellular and ex vivo genital and colorectal tissue explant models. Increased and sustained activity was detected for L'644, a cholesterol-derivatized version of C34, relative to the other FIs. The higher potency of L'644 was further increased with sustained exposure of cells or tissue to the compound. The activity of L'644 was not affected by biological fluids, and the compound was still active when tissue explants were treated after viral exposure. L'644 was also more active than other FIs against a viral escape mutant resistant to reverse transcriptase inhibitors (RTIs), demonstrating the potential of L'644 to be included as part of a multiactive antiretroviral (ARV) combination-based microbicide. These data support the further development of L'644 for microbicide application.
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