ArticleJournal of virology2004
Styrylquinolines, integrase inhibitors acting prior to integration: a new mechanism of action for anti-integrase agents.
Article in Journal of virology, 2004. 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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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
21 citing papers in PubMed, 78 citations in OpenAlex.
- GRL-142 binds to and impairs HIV-1 integrase nuclear localization signal and potently suppresses highly INSTI-resistant HIV-1 variants.Science advances · 2023Article
- HIV‑1 integrase inhibitors targeting various DDE transposases: Retroviral integration versus RAG‑mediated recombination (Review).Molecular medicine reports · 2019Review
- Microwave-assisted, rapid synthesis of 2-vinylquinolines and evaluation of their antimalarial activity.Tetrahedron letters · 2019Article
- Recent advances in the discovery of small-molecule inhibitors of HIV-1 integrase.Future science OA · 2018Review
- Probing Resistance Mutations in Retroviral Integrases by Direct Measurement of Dolutegravir Fluorescence.Scientific reports · 2017Article
- Structural Studies of the HIV-1 Integrase Protein: Compound Screening and Characterization of a DNA-Binding Inhibitor.PloS one · 2015Article
- Design, Synthesis and In Vitro Activity of Anticancer Styrylquinolines. The p53 Independent Mechanism of Action.PloS one · 2015Article
- Multiple genetic pathways involving amino acid position 143 of HIV-1 integrase are preferentially associated with specific secondary amino acid substitutions and confer resistance to raltegravir and cross-resistance to elvitegravir.Antimicrobial agents and chemotherapy · 2013Article
- Allosteric integrase inhibitor potency is determined through the inhibition of HIV-1 particle maturation.Proceedings of the National Academy of Sciences of the United States of America · 2013Article
- Structure-analysis of the HIV-1 integrase Y143C/R raltegravir resistance mutation in association with the secondary mutation T97A.Antimicrobial agents and chemotherapy · 2011Article
- Prospective strategies for targeting HIV-1 integrase function.Future medicinal chemistry · 2010Article
- A cooperative and specific DNA-binding mode of HIV-1 integrase depends on the nature of the metallic cofactor and involves the zinc-containing N-terminal domain.Nucleic acids research · 2010Article
- Chemistry and structure-activity relationship of the styrylquinoline-type HIV integrase inhibitors.Molecules (Basel, Switzerland) · 2010Review
- The HIV-1 integrase mutations Y143C/R are an alternative pathway for resistance to Raltegravir and impact the enzyme functions.PloS one · 2010Article
- HIV-1 IN inhibitors: 2010 update and perspectives.Current topics in medicinal chemistry · 2009Review
- Integrase and integration: biochemical activities of HIV-1 integrase.Retrovirology · 2008Review
- Inhibitors of strand transfer that prevent integration and inhibit human T-cell leukemia virus type 1 early replication.Antimicrobial agents and chemotherapy · 2008Article
- Human immunodeficiency virus type 1 (HIV-1) integration: a potential target for microbicides to prevent cell-free or cell-associated HIV-1 infection.Antimicrobial agents and chemotherapy · 2008Article
- Mutations associated with failure of raltegravir treatment affect integrase sensitivity to the inhibitor in vitro.Antimicrobial agents and chemotherapy · 2008Article
- Dihydroxythiophenes are novel potent inhibitors of human immunodeficiency virus integrase with a diketo acid-like pharmacophore.Journal of virology · 2006Article
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We have previously shown that styrylquinolines (SQLs) are integrase inhibitors in vitro. They compete with the long terminal repeat substrate for integrase. Here, we describe the cellular mode of action of these molecules. We show that SQLs do not interfere with virus entry. In fact, concentrations of up to 20 times the 50% inhibitory concentration did not inhibit cell-to-cell fusion or affect the interaction between GP120 and CD4 in vitro. Moreover, the pseudotype of the retrovirus envelope did not affect drug activity. Quantitative reverse transcription PCR experiments showed that SQLs do not inhibit the entry of the genomic RNA. In contrast, the treatment of human immunodeficiency virus type 1-infected cells with SQLs reduced the amount of the late cDNA, suggesting for the first time that integrase targeting molecules may affect the accumulation of DNA during reverse transcription. The cellular target of SQLs was confirmed by the appearance of mutations in the integrase gene when viruses were grown in the presence of increasing concentrations of SQLs. Finally, these mutations led to SQL-resistant viruses when introduced into the wild-type sequence. In contrast, SQLs were fully active against reverse transcriptase inhibitor- and diketo acid-resistant viruses, positioning SQLs as a second group of anti-integrase compounds.
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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.