ArticleNucleic acids research2020
BMPQ-1 binds selectively to (3+1) hybrid topologies in human telomeric G-quadruplex multimers.
Article in Nucleic acids research, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 27 citations in OpenAlex.
- Rational Polyligand Design for G-Quadruplex Multimer Stabilization.Journal of chemical information and modeling · 2026Article
- Ligands reshape the compactness, stability, and topology of telomeric G-quadruplex dimers.Nucleic acids research · 2026Article
- Revealing G4 Structures as Drug Targets: Exploring the Potential of Novel Therapeutic Agents.Research (Washington, D.C.) · 2026Review
- Higher Selective Targeting of Telomeric Multimeric G-quadruplex by Natural Product Berberine.Current medicinal chemistry · 2026Article
- Guide for phenotype-specific profiling of DNA G-quadruplex-regulated genes.STAR protocols · 2024Review
- EndoQuad: a comprehensive genome-wide experimentally validated endogenous G-quadruplex database.Nucleic acids research · 2024Article
- Insect multimeric G-quadruplexes fold into antiparallel structures of different compactness and stability in KRSC advances · 2023Article
- An automated single-molecule FRET platform for high-content, multiwell plate screening of biomolecular conformations and dynamics.Nature communications · 2023Article
- Effects of Molecular Crowding on the Structure, Stability, and Interaction with Ligands of G-quadruplexes.ACS omega · 2023Review
- RHPS4 shifted the conformation ensemble equilibrium of Tel24 by preferentially stabilizing the (3 + 1) hybrid-2 conformation.RSC advances · 2022Article
- Research Progress on G-Quadruplexes in Human Telomeres and Human Telomerase Reverse Transcriptase (hTERT) Promoter.Oxidative medicine and cellular longevity · 2022Review
- Triazolyl Dibenzo[Asian journal of organic chemistry · 2021Article
- The Binding Pocket at the Interface of Multimeric Telomere G-quadruplexes: Myth or Reality?Chemistry (Weinheim an der Bergstrasse, Germany) · 2021Article
- The solution structures of higher-order human telomere G-quadruplex multimers.Nucleic acids research · 2021Article
Corrections and comments
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Authors and funding
14 authors at 2 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A single G-quadruplex forming sequence from the human telomere can adopt six distinct topologies that are inter-convertible under physiological conditions. This presents challenges to design ligands that show selectivity and specificity towards a particular conformation. Additional complexity is introduced in differentiating multimeric G-quadruplexes over monomeric species, which would be able to form in the single-stranded 3' ends of telomeres. A few ligands have been reported that bind to dimeric quadruplexes, but their preclinical pharmacological evaluation is limited. Using multidisciplinary approaches, we identified a novel quinoline core ligand, BMPQ-1, which bound to human telomeric G-quadruplex multimers over monomeric G-quadruplexes with high selectivity, and induced the formation of G-quadruplex DNA along with the related DNA damage response at the telomere. BMPQ-1 reduced tumor cell proliferation with an IC50 of ∼1.0 μM and decreased tumor growth rate in mouse by half. Biophysical analysis using smFRET identified a mixture of multiple conformations coexisting for dimeric G-quadruplexes in solution. Here, we showed that the titration of BMPQ-1 shifted the conformational ensemble of multimeric G-quadruplexes towards (3+1) hybrid-2 topology, which became more pronounced as further G-quadruplex units are added.
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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 Socratic graph.