Mechanisms of Selectivity of Intercalating Agents

2015 ◽  
pp. 247-254 ◽  
Author(s):  
Herbert S. Schwartz ◽  
G. Schioppacassi ◽  
P. M. Kanter
Keyword(s):  
Intercalating Agents

Carbazole Derivatives as Kinase-Targeting Inhibitors for Cancer Treatment

2020 ◽  
Vol 20 (6) ◽  
pp. 444-465 ◽  
Author(s):  
Jessica Ceramella ◽  
Domenico Iacopetta ◽  
Alexia Barbarossa ◽  
Anna Caruso ◽  
Fedora Grande ◽  
...  
Keyword(s):  
Cancer Progression ◽  
Drug Targets ◽  
Mechanisms Of Action ◽  
Biological Pathways ◽  
G Protein Coupled Receptors ◽  
Ability To Act ◽  
Different Types ◽  
Activity Of Enzymes ◽  
Intercalating Agents ◽  
G Protein Coupled

Protein Kinases (PKs) are a heterogeneous family of enzymes that modulate several biological pathways, including cell division, cytoskeletal rearrangement, differentiation and apoptosis. In particular, due to their crucial role during human tumorigenesis and cancer progression, PKs are ideal targets for the design and development of effective and low toxic chemotherapeutics and represent the second group of drug targets after G-protein-coupled receptors. Nowadays, several compounds have been claimed to be PKs inhibitors, and some of them, such as imatinib, erlotinib and gefitinib, have already been approved for clinical use, whereas more than 30 others are in various phases of clinical trials. Among them, some natural or synthetic carbazole-based molecules represent promising PKs inhibitors due to their capability to interfere with PK activity by different mechanisms of action including the ability to act as DNA intercalating agents, interfere with the activity of enzymes involved in DNA duplication, such as topoisomerases and telomerases, and inhibit other proteins such as cyclindependent kinases or antagonize estrogen receptors. Thus, carbazoles can be considered a promising this class of compounds to be adopted in targeted therapy of different types of cancer.

scholarly journals Nuclear topoisomerase II levels correlate with the sensitivity of mammalian cells to intercalating agents and epipodophyllotoxins.

1988 ◽  
Vol 263 (33) ◽  
pp. 17724-17729
Author(s):  
S M Davies ◽  
C N Robson ◽  
S L Davies ◽  
I D Hickson
Keyword(s):  
Mammalian Cells ◽  
Topoisomerase Ii ◽  
Intercalating Agents

scholarly journals Attenuation of Cytotoxic Natural Product DNA Intercalating Agents by Caffeine

2011 ◽  
Vol 79 (4) ◽  
pp. 729-747 ◽  
Author(s):  
Gabrielle M. Hill
Keyword(s):  
Natural Product ◽  
Intercalating Agents

Characterization of nuclear structures containing superhelical DNA

1976 ◽  
Vol 22 (2) ◽  
pp. 303-324 ◽  
Author(s):  
P.R. Cook ◽  
I.A. Brazell ◽  
E. Jost
Keyword(s):  
Protein Content ◽  
Ionic Detergents ◽  
High Concentrations ◽  
Nuclear Structures ◽  
Intercalating Agents ◽  
Made In

Structures resembling nuclei but depleted of protein may be released by gently lysing cells in solutions containing non-ionic detergents and high concentrations of salt. These nucleoids sediment in gradients containing intercalating agents in a manner characteristic of DNA that is intact, supercoiled and circular. The concentration of salt present during isolation of human nucleoids affects their protein content. When made in I-95 M NaCl they lack histones and most of the proteins characteristic of chromatin; in 1-0 M NaCl they contain variable amounts of histones. The effects of various treatments on nucleoid integrity were investigated.

DNA Binders: 1. Evaluation of DNA-Interactive Ability, Design, and Synthesis of Novel Intercalating Agents

2009 ◽  
Vol 6 (1) ◽  
pp. 56-62 ◽  
Author(s):  
Mario Sechi ◽  
Marco Derudas ◽  
Roberto Dallocchio ◽  
Alessandro Dessì ◽  
Alessia Cosseddu ◽  
...  
Keyword(s):  
Design And Synthesis ◽  
Dna Binders ◽  
Intercalating Agents

Mutagenicity of some intercalating agents in Chinese hamster V79 cells

1984 ◽  
Vol 137 (2-3) ◽  
pp. 117-122 ◽  
Author(s):  
M.R. O'Donovan
Keyword(s):  
Chinese Hamster ◽  
V79 Cells ◽  
Chinese Hamster V79 Cells ◽  
Intercalating Agents

scholarly journals Polypyridyl Ruthenium Complexes: Novel DNA-Intercalating Agents against Human Breast Tumor

2017 ◽  
Author(s):  
João Barolli ◽  
Rodrigo Corrêa ◽  
Fabio Miranda ◽  
Juliana Ribeiro ◽  
Carlos Bloch Jr. ◽  
...  
Keyword(s):  
Breast Tumor ◽  
Ruthenium Complexes ◽  
Human Breast ◽  
Human Breast Tumor ◽  
Intercalating Agents

scholarly journals Enzymatic amplification of translation inhibition of rabbit β-globin mRNA mediated by anti-messenger oligodeoxynucleotides covalently linked to intercalating agents

1987 ◽  
Vol 15 (12) ◽  
pp. 4717-4736 ◽  
Author(s):  
Christian Cazenave ◽  
Nadine Loreau ◽  
Nguyen T. Thuong ◽  
Jean-Jacques Toulmé ◽  
Claude Hélène
Keyword(s):  
Globin Mrna ◽  
Translation Inhibition ◽  
Enzymatic Amplification ◽  
Covalently Linked ◽  
Intercalating Agents

scholarly journals Bifunctional intercalation and sequence specificity in the binding of quinomycin and triostin antibiotics to deoxyribonucleic acid

1978 ◽  
Vol 173 (1) ◽  
pp. 115-128 ◽  
Author(s):  
J S Lee ◽  
M J Waring
Keyword(s):  
Binding Constant ◽  
Binding Constants ◽  
Sequence Specificity ◽  
Peptide Antibiotics ◽  
Naturally Occurring ◽  
Binding Isotherms ◽  
Triostin A ◽  
Specificity Pattern ◽  
Intercalating Agents ◽  
Binding Curves

Quinomycin C, triostin A and triostin C are peptide antibiotics of the quinoxaline family, of which echinomycin (quinomycin A) is also a member. They all remove and reverse the supercoiling of closed circular duplex DNA from bacteriophage PM2 in the fashion characteristic of intercalating drugs, and the unwinding angle at I 0.01 is, in all cases, almost twice that of ethidium. Thus, as with echinomycin, they can be characterized as bifunctional intercalating agents. For the triostins this conclusion has been confirmed by measurements of changes in the viscosity of sonicated rod-like DNA fragments; the helix extension was found to be almost double that expected for a simple monofunctional intercalation process. For triostin A, further evidence for bifunctionality was derived from the cross-over point of binding isotherms to nicked circular and closed circular bacteriophage-PM2DNA. Binding curves for the interaction of quinomycin C and triostin A with a variety of synthetic and naturally occurring nucleic acids were determined by solvent-partition analysis, but triostin C was too insoluble in aqueous solution to make this method applicable. For quinomycin C the highest binding constant was found with Micrococcus lysodeikticus DNA, and its pattern of specificity among natural DNA species was broadly similar to that of echinomycin, although the binding constants were 2–6 times as large. For triostin A the highest binding constant was again found for M. lysodeikticus DNA, but the specificity pattern was quite different from that of the quinomycins. In particular, triostin A bound better to poly(dA-dT) than to the poly(dG-dC) whereas this order was reversed for quinomycin C. There was also evidence that the binding to poly(dA-dT) might be co-operative in nature. No significant interaction could be detected with poly(dA).poly(dT) or with RNA from Escherichia coli. Poly(dG).poly(dC) gave variable results, depending on the source of the polymer. The different patterns of specificity displayed by the quinomycins and triostins are tentatively ascribed to differences in their conformations in solution.

Synthesis of Oligonucleotides Covalently Linked to Intercalating Agents and to Reactive Groups

1991 ◽  
Vol 10 (1-3) ◽  
pp. 359-362 ◽  
Author(s):  
Ulysse Asseline ◽  
Nguyen T. Thuong
Keyword(s):  
Reactive Groups ◽  
Covalently Linked ◽  
Intercalating Agents
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