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5 results on '"Ginnari-Satriani L"'

2. The triazatruxene derivative azatrux binds to the parallel form of the human telomeric G-quadruplex under molecular crowding conditions: biophysical and molecular modeling studies

Author

Luigi Petraccone, Annunziata Cummaro, Stephen Neidle, Ettore Novellino, Shozeb Haider, Luca Ginnari-Satriani, Bruno Pagano, Concetta Giancola, Antonio Randazzo, Iolanda Fotticchia, Petraccone, Luigi, Fotticchia, Iolanda, Cummaro, Annunziata, Pagano, Bruno, Ginnari Satriani, L., Haider, S., Randazzo, Antonio, Novellino, Ettore, Neidle, S., and Giancola, Concetta

Subjects
Models, Molecular, Circular dichroism, Molecular model, Biophysics, Carbazoles, Calorimetry, G-quadruplex, Biochemistry, chemistry.chemical_compound, Piperidines, Humans, heterocyclic compounds, Gene, Chemistry, Circular Dichroism, Isothermal titration calorimetry, General Medicine, DNA, Telomere, Fluorescence, G-Quadruplexes, Spectrometry, Fluorescence, Spectrophotometry, Ultraviolet, Selectivity
Abstract

The present study has employed a combination of spectroscopic, calorimetric and computational methods to explore the binding of the three side-chained triazatruxene derivative, termed azatrux, to a human telomeric G-quadruplex sequence, under conditions of molecular crowding. The binding of azatrux to the tetramolecular parallel [d(TGGGGT)](4) quadruplex in the presence and absence of crowding conditions, was also characterized. The data indicate that azatrux binds in an end-stacking mode to the parallel G-quadruplex scaffold and highlights the key structural elements involved in the binding. The selectivity of azatrux for the human telomeric G-quadruplex relative to another biologically relevant G-quadruplex (c-Kit87up) and to duplex DNA was also investigated under molecular crowding conditions, showing that azatrux has good selectivity for the human telomeric G-quadruplex over the other investigated DNA structures.

Published
2011

3. The triazatruxene derivative azatrux binds to the parallel form of the human telomeric G-quadruplex under molecular crowding conditions: biophysical and molecular modeling studies.

Author

Petraccone L, Fotticchia I, Cummaro A, Pagano B, Ginnari-Satriani L, Haider S, Randazzo A, Novellino E, Neidle S, and Giancola C

Subjects
Biophysics, Calorimetry methods, Circular Dichroism, DNA chemistry, DNA metabolism, Humans, Models, Molecular, Spectrometry, Fluorescence, Spectrophotometry, Ultraviolet, Telomere genetics, Telomere metabolism, Carbazoles chemistry, Carbazoles metabolism, G-Quadruplexes, Piperidines chemistry, Piperidines metabolism
Abstract

The present study has employed a combination of spectroscopic, calorimetric and computational methods to explore the binding of the three side-chained triazatruxene derivative, termed azatrux, to a human telomeric G-quadruplex sequence, under conditions of molecular crowding. The binding of azatrux to the tetramolecular parallel [d(TGGGGT)](4) quadruplex in the presence and absence of crowding conditions, was also characterized. The data indicate that azatrux binds in an end-stacking mode to the parallel G-quadruplex scaffold and highlights the key structural elements involved in the binding. The selectivity of azatrux for the human telomeric G-quadruplex relative to another biologically relevant G-quadruplex (c-Kit87up) and to duplex DNA was also investigated under molecular crowding conditions, showing that azatrux has good selectivity for the human telomeric G-quadruplex over the other investigated DNA structures., (Copyright © 2011 Elsevier Masson SAS. All rights reserved.)

Published
2011
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4. N-cyclic bay-substituted perylene G-quadruplex ligands have selective antiproliferative effects on cancer cells and induce telomere damage.

Author

Casagrande V, Salvati E, Alvino A, Bianco A, Ciammaichella A, D'Angelo C, Ginnari-Satriani L, Serrilli AM, Iachettini S, Leonetti C, Neidle S, Ortaggi G, Porru M, Rizzo A, Franceschin M, and Biroccio A

Subjects
Antineoplastic Agents pharmacology, Cell Line, Tumor, Cell Proliferation drug effects, Cell Survival drug effects, DNA Damage, Drug Screening Assays, Antitumor, Fluorescence Resonance Energy Transfer, Histones metabolism, Humans, Ligands, Perylene pharmacology, Phosphorylation, Piperidines pharmacology, Spectrometry, Mass, Electrospray Ionization, Structure-Activity Relationship, Antineoplastic Agents chemical synthesis, G-Quadruplexes, Perylene analogs & derivatives, Perylene chemical synthesis, Piperidines chemical synthesis, Telomere drug effects
Abstract

A series of bay-substituted perylene derivatives is reported as a new class of G-quadruplex ligands. The synthesized compounds have differing N-cyclic substituents on the bay area and differing side chains on the perylene major axis. ESI-MS and FRET measurements highlighted the strongest quadruplex binders in this series and those showing the highest quadruplex/duplex selectivity. Several biological assays were performed on these compounds, which showed that compound 5 (PPL3C) triggered a DNA damage response in transformed cells with the formation of telomeric foci containing phosphorylated γ-H2AX and 53BP1. This effect mainly occurred in replicating cells and was consistent with Pot1 dissociation. Compound 5 does not induce telomere damage in normal cells, which are unaffected by treatment with the compound, suggesting that this agent preferentially kills cancer cells. These results reinforce the notion that G-quadruplex binding compounds can act as broad inhibitors of telomere-related processes and have potential as selective antineoplastic drugs.

Published
2011
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5. A hydrophilic three side-chained triazatruxene as a new strong and selective G-quadruplex ligand.

Author

Ginnari-Satriani L, Casagrande V, Bianco A, Ortaggi G, and Franceschin M

Subjects
Base Sequence, Binding, Competitive, Carbazoles pharmacology, Cell Line, Tumor, Cell Proliferation drug effects, DNA genetics, Humans, Hydrophobic and Hydrophilic Interactions, Ligands, Models, Molecular, Molecular Conformation, Spectrometry, Mass, Electrospray Ionization, Spectrophotometry, Ultraviolet, Substrate Specificity, Carbazoles chemistry, Carbazoles metabolism, DNA chemistry, DNA metabolism, G-Quadruplexes
Abstract

A new hydrosoluble triazatruxene derivative (Azatrux) is reported to selectively bind to G-quadruplex DNA, as derived by ESI-MS measurements and competition experiments.

Published
2009
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