ArticleNucleic acids research2019
Structures of 1:1 and 2:1 complexes of BMVC and MYC promoter G-quadruplex reveal a mechanism of ligand conformation adjustment for G4-recognition.
Article in Nucleic acids research, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Who cites it
35 citing papers in PubMed, 58 citations in OpenAlex.
- Dual targeting of topoisomerase I and DNA G-quadruplexes enhances senescence and chemosensitivity in colorectal cancer.Communications biology · 2026Article
- High-Sensitivity DNA Aptasensors for Detecting Salivary Biomarker S100A7 in Heart Failure.ACS omega · 2026Article
- Molecular Tools for Precision Targeting and Detection of G-Quadruplex Structures.Molecules (Basel, Switzerland) · 2025Review
- Molecular recognition and effects of a benzothiazole derivative targeting the MYC G-quadruplex.Nucleic acids research · 2025Article
- The interactions of Pu22 G-quadruplex, derived fromMolecular therapy. Nucleic acids · 2025Article
- Atomistic Insights Into Interaction of Doxorubicin With DNA: From Duplex to Nucleosome.Journal of computational chemistry · 2025Article
- Discovery of Palbociclib as a potent c-Myc G4 stabilizer for lung cancer treatment using molecular docking, molecular dynamics simulation, and in vitro activity evaluation.Molecular diversity · 2024Article
- Modeling and NMR Data Elucidate the Structure of a G-Quadruplex-Ligand Interaction for a Pu22T-Cyclometalated Iridium(III) System.The journal of physical chemistry. B · 2024Article
- Solution structures and effects of a platinum compound successively bound MYC G-quadruplex.Nucleic acids research · 2024Article
- Unfolding rates of 1:1 and 2:1 complex of CX-5461 and c-Biophysics reports · 2024Article
- Structural Differences at Quadruplex-Duplex Interfaces Enable Ligand-Induced Topological Transitions.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Comprehensive analysis of intramolecular G-quadruplex structures: furthering the understanding of their formalism.Nucleic acids research · 2024Article
- Recent Advances in Fluorescent Probes for G-quadruplex DNAs / RNAs.Mini reviews in medicinal chemistry · 2024Review
- G-Quadruplexes in Human Telomere: Structures, Properties, and Applications.Molecules (Basel, Switzerland) · 2023Review
- A new G-quadruplex-specific photosensitizer inducing genome instability in cancer cells by triggering oxidative DNA damage and impeding replication fork progression.Nucleic acids research · 2023Article
- G-Quadruplexes in c-MYC Promoter as Targets for Cancer Therapy.Biomedicines · 2023Review
- 4'-SCFAngewandte Chemie (International ed. in English) · 2022Article
- Insights into the Small Molecule Targeting of Biologically Relevant G-Quadruplexes: An Overview of NMR and Crystal Structures.Pharmaceutics · 2022Review
- Structural insight into the bulge-containing KRAS oncogene promoter G-quadruplex bound to berberine and coptisine.Nature communications · 2022Article
- DNA G-Quadruplex in Human Telomeres and Oncogene Promoters: Structures, Functions, and Small Molecule Targeting.Accounts of chemical research · 2022Article
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Authors and funding
6 authors at 4 institutions in 3 countries.
Funding
Abstract
BMVC is the first fluorescent probe designed to detect G-quadruplexes (G4s) in vivo. The MYC oncogene promoter forms a G4 (MycG4) which acts as a transcription silencer. Here, we report the high-affinity and specific binding of BMVC to MycG4 with unusual slow-exchange rates on the NMR timescale. We also show that BMVC represses MYC in cancer cells. We determined the solution structures of the 1:1 and 2:1 BMVC-MycG4 complexes. BMVC first binds the 5'-end of MycG4 to form a 1:1 complex with a well-defined structure. At higher ratio, BMVC also binds the 3'-end to form a second complex. In both complexes, the crescent-shaped BMVC recruits a flanking DNA residue to form a BMVC-base plane stacking over the external G-tetrad. Remarkably, BMVC adjusts its conformation to a contracted form to match the G-tetrad for an optimal stacking interaction. This is the first structural example showing the importance of ligand conformational adjustment in G4 recognition. BMVC binds the more accessible 5'-end with higher affinity, whereas sequence specificity is present at the weaker-binding 3'-site. Our structures provide insights into specific recognition of MycG4 by BMVC and useful information for design of G4-targeted anticancer drugs and fluorescent probes.
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