ArticleScientific reports2015
A G-quadruplex-binding compound showing anti-tumour activity in an in vivo model for pancreatic cancer.
Article in Scientific reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 50 papers.
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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.
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Who cites it
50 citing papers in PubMed, 114 citations in OpenAlex.
- Article
- Binding of Tetrapentylammonium to a c-MYC G-quadruplex Depicted through NMR and Volumetric Assessment.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Review
- G-quadruplex structure in plants and insects and potential applications in pest control.Crop health · 2025Review
- Looping forward: exploring R-loop processing and therapeutic potential.FEBS letters · 2025Review
- A Phenotypic Approach to the Discovery of Potent G-Quadruplex Targeted Drugs.Molecules (Basel, Switzerland) · 2024Review
- Carbazole Derivatives Binding to Bcl-2 Promoter Sequence G-quadruplex.Pharmaceuticals (Basel, Switzerland) · 2024Article
- An Upstream G-Quadruplex DNA Structure Can Stimulate Gene Transcription.ACS chemical biology · 2024Article
- Structure-activity relationships for the G-quadruplex-targeting experimental drug QN-302 and two analogues probed with comparative transcriptome profiling and molecular modeling.Scientific reports · 2024Article
- G-quadruplex structural dynamics at MAPK12 promoter dictates transcriptional switch to determine stemness in breast cancer.Cellular and molecular life sciences : CMLS · 2024Article
- The Epigenomic Features and Potential Functions of PEG- and PDS-Favorable DNA G-Quadruplexes in Rice.International journal of molecular sciences · 2024Article
- Application of G-quadruplex targets in gastrointestinal cancers: Advancements, challenges and prospects.World journal of gastrointestinal oncology · 2023Review
- In vivo dynamics and regulation of DNA G-quadruplex structures in mammals.Cell & bioscience · 2023Review
- Polyamine-Drug Conjugates: Do They Boost Drug Activity?Molecules (Basel, Switzerland) · 2023Review
- G4-quadruplex-binding proteins: review and insights into selectivity.Biophysical reviews · 2022Review
- G-Quadruplex DNA as a Target in Pathogenic Bacteria: Efficacy of an Extended Naphthalene Diimide Ligand and Its Mode of Action.Journal of medicinal chemistry · 2022Article
- Major Achievements in the Design of Quadruplex-Interactive Small Molecules.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Structured Waters Mediate Small Molecule Binding to G-Quadruplex Nucleic Acids.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Identification of Effective Anticancer G-Quadruplex-Targeting Chemotypes through the Exploration of a High Diversity Library of Natural Compounds.Pharmaceutics · 2021Article
- Quadruplex Ligands in Cancer Therapy.Cancers · 2021Review
Corrections and comments
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Authors and funding
15 authors at 3 institutions in 2 countries.
Funding
Abstract
We report here that a tetra-substituted naphthalene-diimide derivative (MM41) has significant in vivo anti-tumour activity against the MIA PaCa-2 pancreatic cancer xenograft model. IV administration with a twice-weekly 15 mg/kg dose produces ca 80% tumour growth decrease in a group of tumour-bearing animals. Two animals survived tumour-free after 279 days. High levels of MM41 are rapidly transported into cell nuclei and were found to accumulate in the tumour. MM41 is a quadruplex-interactive compound which binds strongly to the quadruplexes encoded in the promoter sequences of the BCL-2 and k-RAS genes, both of which are dis-regulated in many human pancreatic cancers. Levels of BCL-2 were reduced by ca 40% in tumours from MM41-treated animals relative to controls, consistent with BCL-2 being a target for MM41. Molecular modelling suggests that MM41 binds to a BCL-2 quadruplex in a manner resembling that previously observed in co-crystal structures with human telomeric quadruplexes. This supports the concept that MM41 (and by implication other quadruplex-targeting small molecules) can bind to quadruplex-forming promoter regions in a number of genes and down-regulate their transcription. We suggest that quadruplexes within those master genes that are up-regulated drivers for particular cancers, may be selective targets for compounds such as MM41.
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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.