A series of N-monosubstituted and N,N'-disubstituted derivatives of the indolo[3,2-b]carbazole chromophore have been prepared, and their binding affinity for duplex DNA has been evaluated by ultraviolet and fluorescence spectroscopies. It has been found that indolo[3,2-b]carbazoles bearing basic N-alkyl substituents are intercalators that bind DNA with affinities in the micromolar and submicromolar range and a preference for associating with sequences of mixed composition and purine-pyrimidine steps.
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http://dx.doi.org/10.1039/c4ob02566k | DOI Listing |
Methods Mol Biol
January 2025
Department of Pharmacology, Yale School of Medicine, Yale University, New Haven, CT, USA.
Electrophoretic Mobility Shift Assay (EMSA) is a powerful technique for studying nucleic acid and protein interactions. This technique is based on the principle that nucleic acid-protein complex and nucleic acid migrate at different rates due to differences in size and charge. Nucleic acid and protein interactions are fundamental to various biological processes, such as gene regulation, replication, transcription, and recombination.
View Article and Find Full Text PDFAppl Environ Microbiol
December 2024
Department of Microbiology, Harvard Medical School, Boston, Massachusetts, USA.
is an obligate anaerobic, Gram-positive bacterium that produces toxins. Despite technological progress, conducting gene expression analysis of under different conditions continues to be labor-intensive. Therefore, there is a demand for simplified tools to investigate the transcriptional and translational regulation of .
View Article and Find Full Text PDFJ Virol
December 2024
Department of Microbiology and Immunology, University of Michigan, Ann Arbor, Michigan, USA.
Protein kinase R (PKR) is an interferon-induced antiviral protein activated by autophosphorylation in response to double strand DNA (dsRNA) and other stimuli. Activated PKR causes translation inhibition and apoptosis, and it contributes to proinflammatory responses, cell growth, and differentiation. Mouse adenovirus type 1 (MAV-1) counteracts PKR by causing its degradation via a viral protein, early region 4 open reading frame 6 (E4orf6).
View Article and Find Full Text PDFChem Biodivers
January 2025
Guangxi Science and Technology Normal University, School of food biochemical engineering, Tiebei road 966, 546199, Laibin, CHINA.
Although cisplatin is widely used as a first-line chemotherapy agent, it has significant side effects. Herein, we synthesized a Pt(II) complex (Pt1) derived from o-vanillin-4-phenylthiosemicarbazone ligand, and confirmed its crystal structure by X-ray crystallography. Complex Pt1 exhibited potent anticancer activity against various tested cancer cell lines, with particular efficacy against HepG-2 cells.
View Article and Find Full Text PDFJ Med Chem
January 2025
SANKEN, Osaka University, Mihogaoka, Ibaraki-shi, Osaka 567-0047, Japan.
Histone methylation, a crucial aspect of epigenetics, intricately involves specialized enzymes such as G9a, a histone methyltransferase (HMT) catalyzing the methylation of histone H3 lysine 9 (H3K9) and H3K27. Apart from histone modification, G9a regulates essential cellular processes such as deoxyribonucleic acid (DNA) replication, damage repair, and gene expression via modulating DNA methylation patterns. The dysregulation and overexpression of G9a are intricately linked to cancer initiation, progression, and metastasis, making it a compelling target for anticancer therapy.
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