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DNA intercalation

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https://www.readbyqxmd.com/read/28231533/synthesis-characterization-and-dna-binding-cleavage-protein-binding-and-cytotoxicity-studies-of-co-ii-ni-ii-cu-ii-and-zn-ii-complexes-of-aminonaphthoquinone
#1
A Kosiha, C Parthiban, Kuppanagounder P Elango
The Co(II), Ni(II), Cu(II) and Zn(II) complexes of an aminonaphthoquinone ligand (L) have been prepared and characterized using analytical and spectral techniques. The structures of L and its Zn(II) complex are confirmed by single crystal X-ray diffraction study. The results indicate that Co(II), Ni(II) and Zn(II) complexes possess tetrahedral geometry while Cu(II) complex exhibits square planar structure. The interaction of L and its complexes with CT-DNA reveal that they could interact with CT-DNA through intercalation...
February 16, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28231499/surfactant-cobalt-iii-complexes-the-impact-of-hydrophobicity-on-interaction-with-hsa-and-dna-insights-from-experimental-and-theoretical-approach
#2
Selvakumar Veeralakshmi, Gopal Sabapathi, Selvan Nehru, Ponnambalam Venuvanalingam, Sankaralingam Arunachalam
To develop surfactant-based metallodrugs, it is very important to know about their hydrophobicity, micelle forming capacity, their interaction with biomacromolecules such as proteins and nucleic acids, and biological activities. Here, diethylenetriamine (dien) and tetradecylamine ligand (TA) based surfactant-cobalt(III) complexes with single chain domain, [Co(dien)(TA)Cl2]ClO4 (1) and double chain domain [Co(dien)(TA)2Cl](ClO4)2 (2) were chosen to study the effect of hydrophobicity on the interaction with human serum albumin and calf thymus DNA...
February 16, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28231454/zinc-complexes-of-diflunisal-synthesis-characterization-structure-antioxidant-activity-and-in-vitro-and-in-silico-study-of-the-interaction-with-dna-and-albumins
#3
Alketa Tarushi, Chrisoula Kakoulidou, Catherine P Raptopoulou, Vassilis Psycharis, Dimitris P Kessissoglou, Ioanna Zoi, Athanasios N Papadopoulos, George Psomas
From the reaction of ZnCl2 with the non-steroidal anti-inflammatory drug diflunisal (Hdifl), complex [Zn(difl-O)2(MeOH)4], 1 was formed, while in the presence of a N,N'-donor heterocyclic ligand 2,2'-bipyridylamine (bipyam), 2,2'-bipyridine (bipy), 1,10-phenanthroline (phen) and 2,2'-dipyridylketone oxime (Hpko), the complexes [Zn(difl-O,O')2(bipyam)], 2, [Zn(difl-O,O')2(bipy)], 3, [Zn(difl-O,O')2(phen)], 4 and [Zn(difl-O)2(Hpko)2], 5 were isolated, respectively. The complexes were characterized by physicochemical and spectroscopic techniques and the crystal structures of complexes 2, 3 and 5 were determined by X-ray crystallography...
February 12, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/28224358/synthesis-characterization-and-dna-binding-studies-of-hydroxyl-functionalized-platinum-ii-salphen-complexes
#4
Shahratul Ain Mohd Sukri, Lee Yook Heng, Nurul Huda Abd Karim
The platinum(II) salphen complex N,N'-Bis-4-(hydroxysalicylidene)-phenylenediamine-platinum(II); (1) and its two derivatives containing hydroxyl functionalized side chains N,N'-bis-[4-[[1-(2-hydroxyethoxy)] salicylidene] phenylenediamine-platinum(II); (2) and N,N'-bis-[4-[[1-(3-hydroxypropoxy)] salicylidene] phenylenediamine-platinum(II); (3) were synthesized and characterized. The structures of the complexes were confirmed by (1)H and (13)C NMR spectroscopy, FTIR, ESI-MS and CHN elemental analyses. The effects of the hydroxyl substituent on the spectral properties and the DNA binding behaviors of the Pt(II) complexes were explored...
February 21, 2017: Journal of Fluorescence
https://www.readbyqxmd.com/read/28222362/quinazolinone-benzimidazole-conjugates-synthesis-characterization-dihydrofolate-reductase-inhibition-dna-and-protein-binding-properties
#5
Prinka Singla, Vijay Luxami, Kamaldeep Paul
Quinazolinone and benzimidazole represent as important and abundant classes of fused nitrogen-containing heterocycle. A series of two isomeric quinazolinone-benzimidazole conjugates is synthesized and substitutes with different aromatic rings. These compounds are well characterized by (1)H and (13)C NMR as well as mass spectrometry. Compounds are then evaluated by dihydrofolate reductase inhibitory activity. In vitro assay shows that some compounds are exhibiting significant dihydrofolate reductase inhibitory activities...
February 14, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28215644/from-molecular-insight-to-therapeutic-strategy-the-holistic-approach-for-treating-triple-negative-breast-cancer
#6
REVIEW
Rittwika Bhattacharya, Koyel Banerjee, Nupur Mukherjee, Minakshi Sen, Ashis Mukhopadhyay
Aim of the present study was to analyze the molecular pathogenesis of TNBC, therapeutic practice, challenges, and future goals in treatment strategies. Based on the alterations of distinct pathways, Lehmann's subgroups of TNBCs were further categorized. Those with defective DNA damage repair and replication pathways, viz. Basal Like 1 & 2 (BL1, BL2) were found susceptible to DNA intercalating drugs while those with upregulated cell signalling & motility (mesenchymal (M), mesemchymal stem like (MSL)), cell survival (BL2, M, MSL), angiogenesis (BL2, MSL), T cell signalling (Immunomodulatory/IM) pathways required targeted therapies...
January 19, 2017: Pathology, Research and Practice
https://www.readbyqxmd.com/read/28213325/carbon-dots-based-fret-for-the-detection-of-dna-damage
#7
Jiri Kudr, Lukas Richtera, Kledi Xhaxhiu, David Hynek, Zbynek Heger, Ondrej Zitka, Vojtech Adam
Here, we aimed our attention at the synthesis of carbon dots (C-dots) with the ability to interact with DNA to suggest an approach for the detection of DNA damage. Primarily, C-dots modified with amine moieties were synthesized using the one-step microwave pyrolysis of citric acid in the presence of diethylenetriamine. The C-dots showed strong photoluminescence with a quantum yield of 4%. In addition, the C-dots (2.8±0.8nm) possessed a good colloidal stability and exhibited a positive surface charge (ζ=36mV) at a neutral pH...
February 9, 2017: Biosensors & Bioelectronics
https://www.readbyqxmd.com/read/28211920/evaluation-of-acridine-orange-derivatives-as-dna-targeted-radiopharmaceuticals-for-auger-therapy-influence-of-the-radionuclide-and-distance-to-dna
#8
Edgar Pereira, Letícia do Quental, Elisa Palma, Maria Cristina Oliveira, Filipa Mendes, Paula Raposinho, Isabel Correia, João Lavrado, Salvatore Di Maria, Ana Belchior, Pedro Vaz, Isabel Santos, António Paulo
A new family of (99m)Tc(I)- tricarbonyl complexes and (125)I-heteroaromatic compounds bearing an acridine orange (AO) DNA targeting unit was evaluated for Auger therapy. Characterization of the DNA interaction, performed with the non-radioactive Re and (127)I congeners, confirmed that all compounds act as DNA intercalators. Both classes of compounds induce double strand breaks (DSB) in plasmid DNA but the extent of DNA damage is strongly dependent on the linker between the Auger emitter ((99m)Tc or (125)I) and the AO moiety...
February 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28207251/cross-linked-micellar-spherical-nucleic-acids-from-thermoresponsive-templates
#9
Resham J Banga, Brian Meckes, Suguna P Narayan, Anthony J Sprangers, SonBinh T Nguyen, Chad A Mirkin
A one-pot synthesis of micellar spherical nucleic acid (SNA) nanostructures using Pluronic F127 as a thermoresponsive template is reported. These novel constructs are synthesized in a chemically straightforward process that involves intercalation of the lipid tails of DNA amphiphiles (CpG motifs for TLR-9 stimulation) into the hydrophobic regions of Pluronic F127 micelles followed by chemical cross-linking and subsequent removal of non-crosslinked structures. The dense nucleic acid shell of the resulting cross-linked micellar SNA enhances their stability in physiological media and facilitates their rapid cellular internalization making them effective TLR-9 immunomodulatory agents...
February 16, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28197310/novel-18-f-labeled-1-hydroxyanthraquinone-derivatives-for-necrotic-myocardium-imaging
#10
Ai-Yan Ji, Qiao-Mei Jin, Dong-Jian Zhang, Hua Zhu, Chang Su, Xing-Hua Duan, Li Bian, Zi-Ping Sun, Yi-Cheng Ni, Jian Zhang, Zhi Yang, Zhi-Qi Yin
Rapid detection and precise evaluation of myocardial viability is necessary to aid in clinical decision making whether to recommend revascularization for patients with myocardial infarction (MI). Three novel (18)F-labeled 1-hydroxyanthraquinone derivatives were synthesized, characterized, and evaluated as potential necrosis avid imaging agents for assessment of myocardial viability. Among these tracers, [(18)F]FA3OP emerged as the most promising compound with best stability and highest targetability. Clear PET images of [(18)F]FA3OP were obtained in rat model of myocardial infarction and reperfusion at 1 h after injection...
February 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28196064/mt4-mmp-and-egfr-expression-levels-are-key-biomarkers-for-breast-cancer-patient-response-to-chemotherapy-and-erlotinib
#11
Cassandre Yip, Pierre Foidart, Joan Somja, Alice Truong, Mehdi Lienard, Emilie Feyereisen, Hélène Schroeder, Stéphanie Gofflot, Anne-Françoise Donneau, Joëlle Collignon, Philippe Delvenne, Nor Eddine Sounni, Guy Jerusalem, Agnès Noël
BACKGROUND: Triple-negative breast cancers (TNBC) are heterogeneous cancers with poor prognosis. We aimed to determine the clinical relevance of membrane type-4 matrix metalloproteinase (MT4-MMP), a membrane type matrix metalloproteinase that interacts with epidermal growth factor receptor (EGFR) overexpressed in >50% of TNBC. METHODS: We conducted a retrospective immunohistochemical analysis on human TNBC samples (n=81) and validated our findings in in vitro and in vivo assays...
February 14, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/28192709/tetrazolylmethyl-quinolines-design-docking-studies-synthesis-anticancer-and-antifungal-analyses
#12
Saba Kauser J Shaikh, Ravindra R Kamble, Shilpa M Somagond, H C Devarajegowda, Sheshagiri R Dixit, Shrinivas D Joshi
A new series of 2,5 and 1,5-regioisomers of the tetrazolyl group viz., 3-[(5-benzyl/benzylthio-2H-tetrazol-2-yl) methyl]-2-chloro-6-substituted quinoline 6h-q and 3-[(5-benzyl/benzylthio-1H-tetrazol-1-yl) methyl]-2-chloro-6-substituted quinolines 7h-q were synthesized. Docking studies of all these compounds with DNA as target using PDB: 1AU5 and 453D revealed that the compounds 6h and 6i act as covalent cross linker on the DNA helix of the former and intercalate the latter both with higher C score values. Another set of docking studies in the active pocket of dihydrofolate reductase and N-myristoyl transferase as targets to assess antifungal activity revealed that compounds 6k, 6l, 6p and 7q (with bromo and fluro substituents) showcases different binding modes and hydrogen bonding...
February 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28182434/a-model-based-approach-to-assessing-the-importance-of-intracellular-binding-sites-in-doxorubicin-disposition
#13
Ilse R Dubbelboer, Elsa Lilienberg, Erik Sjögren, Hans Lennernäs
Doxorubicin is an anticancer agent, which binds reversibly to topoisomerase I and II, intercalates to DNA base pairs, and generates free radicals. Doxorubicin has a high tissue:plasma partition coefficient and high intracellular binding to the nucleus and other subcellular compartments. The metabolite doxorubicinol has an extensive tissue distribution. This porcine study investigated whether the traditional implementation of tissue binding, described by the tissue:plasma partition coefficient (Kp,t), could be used to appropriately analyze and/or simulate tissue doxorubicin and doxorubicinol concentrations in healthy pigs, when applying a physiologically based pharmacokinetic (PBPK) model approach, or whether intracellular binding is required in the semi-PBPK model...
February 23, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28178588/investigation-of-the-complex-structure-comparative-dna-binding-and-dna-cleavage-of-two-water-soluble-mono-nuclear-lanthanum-iii-complexes-and-cytotoxic-activity-of-chitosan-coated-magnetic-nanoparticles-as-drug-delivery-for-the-complexes
#14
Zahra Asadi, Neda Nasrollahi, Hamidreza Karbalaei-Heidari, Vaclav Eigner, Michal Dusek, Nabiallah Mobaraki, Roya Pournejati
Two water-soluble mono-nuclear macrocyclic lanthanum(III) complexes of 2,6-diformyl-4-methylphenol with 1,3-diamino-2-propanol (C1) or 1,3-propylenediamine (C2) were synthesized and characterized by UV-Vis, FT-IR, (13)C and (1)H NMR spectroscopy and elemental analysis. C1 complex was structurally characterized by single-crystal X-ray diffraction, which revealed that the complex was mononuclear and ten-coordinated. The coordination sites around lanthanum(III) were occupied with a five-dentate ligand, two bidentate nitrates, and one water molecule...
January 21, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28176928/n-3-hydroxymethyl-%C3%AE-carboline-1-yl-ethyl-2-yl-l-phe-development-toward-a-nanoscaled-antitumor-drug-capable-of-treating-complicated-thrombosis-and-inflammation
#15
Jianhui Wu, Ming Zhao, Yuji Wang, Yaonan Wang, Haimei Zhu, Shurui Zhao, Lin Gui, Xiaoyi Zhang, Shiqi Peng
It is well documented that the surfaces of cancer cells, activated platelets and inflammatory cells are rich in P-selectin. N-(3-hydroxymethyl-β-carboline-1-yl-ethyl-2-yl)-l-Phe (HMCEF) is a P-selectin inhibitor capable of simultaneously inhibiting thrombosis and inflammation. Based on the knowledge that P-selectin is a common target for antithrombotic, anti-inflammatory and antitumor drugs, the aim of this study article was to estimate the possibility of HMCEF as a nanoscaled antitumor drug. Images of transmission electron micro scopy, scanning electron microscopy and atomic force microscopy proved that HMCEF forms nanoparticles with a diameter of <120 nm that promote delivery in blood circulation...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28176860/massively-parallel-digital-high-resolution-melt-for-rapid-and-absolutely-quantitative-sequence-profiling
#16
Daniel Ortiz Velez, Hannah Mack, Julietta Jupe, Sinead Hawker, Ninad Kulkarni, Behnam Hedayatnia, Yang Zhang, Shelley Lawrence, Stephanie I Fraley
In clinical diagnostics and pathogen detection, profiling of complex samples for low-level genotypes represents a significant challenge. Advances in speed, sensitivity, and extent of multiplexing of molecular pathogen detection assays are needed to improve patient care. We report the development of an integrated platform enabling the identification of bacterial pathogen DNA sequences in complex samples in less than four hours. The system incorporates a microfluidic chip and instrumentation to accomplish universal PCR amplification, High Resolution Melting (HRM), and machine learning within 20,000 picoliter scale reactions, simultaneously...
February 8, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28171832/design-and-synthesis-of-novel-phenyl-1-4-beta-carboline-hybrid-molecules-as-potential-anticancer-agents
#17
S Samundeeswari, Bahubali Chougala, Megharaja Holiyachi, Lokesh Shastri, Manohar Kulkarni, Suneel Dodamani, Sunil Jalalpur, Shrinivas Joshi, Sheshagiri Dixit, Vinay Sunagar, Ravindra Hunnur
A series of beta-carbolines with other heterocycles linked by phenyl ring has been designed and synthesized. The key intermediates 3 and 5 were synthesized by condensing tryptamine and teraldehyde via Pictet- Spengler method. All the newly synthesized compounds were tested for their anticancer activity against sixty human cell lines at NCI. The five dose results of compounds 3 and 7a showed enhancement of anticancer activity (GI50 values range from 1.00 to 7.10 μM) against all the cell lines in comparison with some of earlier molecules...
January 11, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28167835/magnetoresistive-sensors-for-measurements-of-dna-hybridization-kinetics-effect-of-tina-modifications
#18
G Rizzi, M Dufva, M F Hansen
We present the use of magnetoresistive sensors integrated in a microfluidic system for real-time studies of the hybridization kinetics of DNA labeled with magnetic nanoparticles to an array of surface-tethered probes. The nanoparticles were magnetized by the magnetic field from the sensor current. A local negative reference ensured that only the specific binding signal was measured. Analysis of the real-time hybridization using a two-compartment model yielded both the association and dissociation constants kon, and koff...
February 7, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28167125/pma-lamp-for-rapid-detection-of-escherichia-coli-and-shiga-toxins-from-viable-but-non-culturable-state
#19
Muxia Yan, Ling Xu, Hua Jiang, Zhenwen Zhou, Shishui Zhou, Li Zhang
In exposure to outer pressure, microorganisms are capable of entry into the Viable But Non-Culturable (VBNC) state, and thus survive under various elimination processing. The survival microorganisms may yield negative results on culturing, and cause false negative for this golden standard methodology. In this study, a novel PMA-LAMP assay on the detection of Enterohemorrhage E. coli and shiga toxins has been developed and evaluated, with further application on a number of food borne E. coli strains. LAMP primers were designed on the target of rfbe for Enterohemorrhage E...
February 3, 2017: Microbial Pathogenesis
https://www.readbyqxmd.com/read/28165751/dna-nanostructure-sequence-dependent-binding-of-organophosphates
#20
Yingning Gao, Samson Or, Aaron Toop, Ian Wheeldon
Understanding the molecular interactions between small molecules and double-stranded DNA has important implications on the design and development of DNA and DNA-protein nanomaterials. Such materials can be assembled into a vast array of 1-, 2-, and 3D structures that contain a range of chemical and physical features where small molecules can bind via intercalation, groove binding, and electrostatics. In this work, we use a series of simulation-guided binding assays and spectroscopy techniques to investigate the binding of selected organophosphtates, methyl parathion, paraoxon, their common enzyme hydrolysis product p-nitrophenol, and double-stranded DNA fragments and DNA DX tiles, a basic building block of DNA-based materials...
February 16, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
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