A set of Ru(ii) metallopeptides containing the dppz ligand has been synthesized using SPPS methods. Fluorescence titration studies show that those metallopeptides featuring an octaarginine tail display a large binding preference for DNA G-quadruplex structures over those lacking it, and also that the interplay between the octoarginine functionalization and the ancillary ligand in the complex has an essential role in the recognition process. Furthermore, the oligoarginine metallopeptides are also efficiently internalized, causing cell death with signs of apoptosis.
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http://dx.doi.org/10.1039/c7cc08286j | DOI Listing |
ACS Appl Bio Mater
January 2025
Department of Chemistry and Biochemistry, Thapar Institute of Engineering and Technology, Patiala 147001, India.
c-Myc is a transcription factor that is overexpressed in most human cancers. Despite its challenging nature, we have developed a series of naphthalimide-imidazopyrazine conjugates to target c-Myc. The library of synthesized derivatives was tested for their anticancer activity against a nine-panel of cancer cell lines.
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January 2025
Department of Chemical and Biological Engineering, Andong National University, Andong, Republic of Korea.
Here, we developed a novel, cost-effective fluorescence light-up biosensor for Pb detection based on a label-free G-quadruplex combined with modified thioflavin T (ThT) derivatives. Among the various G-quadruplex sequences tested, only T2 exhibited fluorescence light-up properties upon interacting with the modified ThT derivatives in the presence of Pb. To enhance the Pb sensing system, we also compared modified ThT derivatives, including the newly synthesized propyl-substituted ThT (ThT-P) and butyl-substituted ThT (ThT-B).
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January 2025
Key Laboratory of the Ministry of Education for Advanced Catalysis Materials, College of Chemistry and Materials Science, Zhejiang Normal University, Jinhua 321004, China.
DNA structures with the potential to concurrently recruit multiple ligands are promising in pharmaceutical and sensing applications when concentrated in a local environment. Herein, we found that human telomeric G-quadruplex (htG4) structures with a junction can selectively aggregate a natural ligand of tetrahydropalmatine (THP) into AIEgens. The htG4 monomer favors formation of a THP dimer emitting at ∼525 nm.
View Article and Find Full Text PDFNucleic Acids Res
January 2025
Department of Molecular Medicine, University of Padua, via A. Gabelli 63, 35121 Padua, Italy.
i-Motifs (iMs) are quadruplex nucleic acid conformations that form in cytosine-rich regions. Because of their acidic pH dependence, iMs were thought to form only in vitro. The recent development of an iM-selective antibody, iMab, has allowed iM detection in cells, which revealed their presence at gene promoters and their cell cycle dependence.
View Article and Find Full Text PDFJ Med Chem
January 2025
Guangdong Medicine-Engineering Interdisciplinary Technology Research Center, School of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou 510006, China.
Positron emission tomography (PET) is a common imaging technique and can provide accurate information about the size, shape, and location of tumors. Recent evidence has shown that G-quadruplex structures (G4s) are identified in human oncogenes, and these special structures are recognized as diagnostic cancer markers and drug targets for anticancer therapies. Although a number of techniques for in vivo imaging of G4s have been developed, achieving sufficient sensitivity and selectivity in vivo remains challenging.
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