ArticleJournal of medicinal chemistry2013
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 102 papers.
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Who cites it
102 citing papers in PubMed, 190 citations in OpenAlex.
- Regulatory roles of G-quadruplexes and G-quadruplex-binding proteins across the enhancer and promoter of the HBV genome.Virology journal · 2026Article
- Investigation of possible G-quadruplex formation by GU- and GA-rich repeats and their role in translation.RNA biology · 2025Article
- Review
- Catalyzing Protein Folding by Chaperones.Biology · 2025Review
- A high-throughput approach to evaluating NCp7 RNA binding activity for HIV-1 drug discovery.SLAS discovery : advancing life sciences R & D · 2025Article
- Rapid G4 Ligand Screening Through Spectral Changes Using HT-SRCD with Minimal Material.Molecules (Basel, Switzerland) · 2025Article
- Viral hijacking of host DDX60 promotes Crimean-Congo haemorrhagic fever virus replication via G-quadruplex unwinding.PLoS pathogens · 2025Article
- Review
- Asymmetric distribution of G-quadruplex forming sequences in genomes of retroviruses.Scientific reports · 2025Article
- Structural elucidation of HIV-1 G-quadruplexes in a cellular environment and their ligand binding using responsiveChemical science · 2024Article
- Base pair dynamics, electrostatics, and thermodynamics at the LTR-III quadruplex:duplex junction.Biophysical journal · 2024Article
- Naphthalene Diimide-Tetraazacycloalkane Conjugates Are G-Quadruplex-Based HIV-1 Inhibitors with a Dual Mode of Action.ACS infectious diseases · 2024Article
- G-Quadruplexes in the Regulation of Viral Gene Expressions and Their Impacts on Controlling Infection.Pathogens (Basel, Switzerland) · 2024Review
- Article
- G-Quadruplexes in the Viral Genome: Unlocking Targets for Therapeutic Interventions and Antiviral Strategies.Viruses · 2023Review
- Unfolding of an RNA G-quadruplex motif in the negative strand genome of porcine reproductive and respiratory syndrome virus by host and viral helicases to promote viral replication.Nucleic acids research · 2023Article
- WebTetrado: a webserver to explore quadruplexes in nucleic acid 3D structures.Nucleic acids research · 2023Article
- G-quadruplex ligands as potent regulators of lysosomes.Autophagy · 2023Article
- DNA topoisomerase 1 represses HIV-1 promoter activity through its interaction with a guanine quadruplex present in the LTR sequence.Retrovirology · 2023Review
- Effects of Molecular Crowding on the Structure, Stability, and Interaction with Ligands of G-quadruplexes.ACS omega · 2023Review
42 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 2 countries.
Funding
Abstract
G-Quadruplexes, noncanonical nucleic acid structures, act as silencers in the promoter regions of human genes; putative G-quadruplex forming sequences are also present in promoters of other mammals, yeasts, and prokaryotes. Here we show that also the HIV-1 LTR promoter exploits G-quadruplex-mediated transcriptional regulation with striking similarities to eukaryotic promoters and that treatment with a G-quadruplex ligand inhibits HIV-1 infectivity. Computational analysis on 953 HIV-1 strains substantiated a highly conserved G-rich sequence corresponding to Sp1 and NF-κB binding sites. Biophysical/biochemical analysis proved that two mutually exclusive parallel-like intramolecular G-quadruplexes, stabilized by small molecule ligands, primarily fold in this region. Mutations disrupting G-quadruplex formation enhanced HIV promoter activity in cells, whereas treatment with a G-quadruplex ligand impaired promoter activity and displayed antiviral effects. These findings disclose the possibility of inhibiting the HIV-1 LTR promoter by G-quadruplex-interacting small molecules, providing a new pathway to development of anti-HIV-1 drugs with unprecedented mechanism of action.
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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.