ArticleJournal of virology2017
Discovery of Novel Small-Molecule Inhibitors of LIM Domain Kinase for Inhibiting HIV-1.
Article in Journal of virology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 41 citations in OpenAlex.
- Cofilin hyperactivation in HIV infection and targeting the cofilin pathway using an anti-αScience advances · 2019Trial
- MELK inhibition disrupts actin cytoskeleton and broadly restricts human coronavirus infections.Nature communications · 2026Article
- Discovery of actinators, actin-derived bioactive peptides that modulate cytoskeleton and actin-related cellular activities.Science advances · 2026Article
- HSV-1 infection induces brain cofilin hyperphosphorylation in the 5×FAD Alzheimer's Disease mouse model.bioRxiv : the preprint server for biology · 2025Article
- Rottlerin inhibits macropinocytosis of Porcine Reproductive and Respiratory Syndrome Virus through the PKCδ-Cofilin signaling pathway.PloS one · 2025Article
- RNA-RNA interactions between respiratory syncytial virus and miR-26 and miR-27 are associated with regulation of cell cycle and antiviral immunity.Nucleic acids research · 2024Article
- Inhibiting F-Actin Polymerization Impairs the Internalization ofMicroorganisms · 2024Article
- Discovery of Ten Anti-HIV Hit Compounds and Preliminary Pharmacological Mechanisms StudiesCurrent HIV research · 2024Article
- Article
- Role of ROCK signaling in virus replication.Virus research · 2023Review
- The Antiviral Compound PSP Inhibits HIV-1 Entry via PKR-Dependent Activation in Monocytic Cells.Viruses · 2023Article
- LIM Kinases, LIMK1 and LIMK2, Are Crucial Node Actors of the Cell Fate: Molecular to Pathological Features.Cells · 2023Review
- Advances in the Development of Small Molecule Antivirals against Equine Encephalitic Viruses.Viruses · 2023Review
- Comparative miRNA transcriptomics of macaques and mice revealsEmerging microbes & infections · 2022Article
- LIM Kinases, Promising but Reluctant Therapeutic Targets: Chemistry and Preclinical Validation In Vivo.Cells · 2022Review
- SARS-CoV-2 3CLpro whole human proteome cleavage prediction and enrichment/depletion analysis.Computational biology and chemistry · 2022Article
- Estradiol inhibits HIV-1Scientific reports · 2022Article
- Prestimulation of CD2 confers resistance to HIV-1 latent infection in blood resting CD4 T cells.iScience · 2021Article
- IP-10 Promotes Latent HIV Infection in Resting Memory CD4Frontiers in immunology · 2021Article
- Hsp90 Inhibitors Inhibit the Entry of Herpes Simplex Virus 1 Into Neuron Cells by Regulating Cofilin-Mediated F-Actin Reorganization.Frontiers in microbiology · 2021Article
Corrections and comments
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Authors and funding
27 authors at 9 institutions in 2 countries.
Funding
Abstract
A dynamic actin cytoskeleton is necessary for viral entry, intracellular migration, and virion release. For HIV-1 infection, during entry, the virus triggers early actin activity by hijacking chemokine coreceptor signaling, which activates a host dependency factor, cofilin, and its kinase, the LIM domain kinase (LIMK). Although knockdown of human LIM domain kinase 1 (LIMK1) with short hairpin RNA (shRNA) inhibits HIV infection, no specific small-molecule inhibitor of LIMK has been available. Here, we describe the design and discovery of novel classes of small-molecule inhibitors of LIMK for inhibiting HIV infection. We identified R10015 as a lead compound that blocks LIMK activity by binding to the ATP-binding pocket. R10015 specifically blocks viral DNA synthesis, nuclear migration, and virion release. In addition, R10015 inhibits multiple viruses, including Zaire ebolavirus (EBOV), Rift Valley fever virus (RVFV), Venezuelan equine encephalitis virus (VEEV), and herpes simplex virus 1 (HSV-1), suggesting that LIMK inhibitors could be developed as a new class of broad-spectrum antiviral drugs.
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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.