Search results for " G-quadruplex DNA"

showing 2 items of 2 documents

Development of Polyamine‐Substituted Triphenylamine Ligands with High Affinity and Selectivity for G‐Quadruplex DNA

2019

Currently, significant efforts are devoted to designing small molecules able to bind selectively to guanine quadruplexes (G4s). These noncanonical DNA structures are implicated in various important biological processes and have been identified as potential targets for drug development. Previously, a series of triphenylamine (TPA)-based compounds, including macrocyclic polyamines, that displayed high affinity towards G4 DNA were reported. Following this initial work, herein a series of second-generation compounds, in which the central TPA has been functionalised with flexible and adaptive linear polyamines, are presented with the aim of maximising the selectivity towards G4 DNA. The acid-bas…

Biochemistry & Molecular BiologyCircular dichroismChemistry Medicinal0601 Biochemistry and Cell BiologyLigands010402 general chemistryTriphenylamineG-quadruplex01 natural sciencesBiochemistryFluorescence spectroscopyStructure-Activity Relationshipchemistry.chemical_compoundFluorescence Resonance Energy TransferPolyaminesPharmacology & PharmacyCOORDINATION CHEMISTRYPROBEMolecular BiologyScience & Technology0304 Medicinal and Biomolecular Chemistry010405 organic chemistryOrganic ChemistryDNACombinatorial chemistrySmall molecule0104 chemical sciences* G-quadruplex DNA * G4 selectivity * polyamine-based ligand *fluorescenceG-QuadruplexesFörster resonance energy transferchemistryDrug DesignFRETEQUILIBRIUM-CONSTANTSMolecular MedicineCOMPLEXESfluorescenceEMISSIONSelectivityLife Sciences & BiomedicineDNAChemBioChem
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The Right Answer for the Right Electrostatics: Force Field Methods Are Able to Describe Relative Energies of DNA Guanine Quadruplexes

2014

Different force fields and approximate density functional theory were applied in order to study the rotamer space of the telomeric G-quadruplex DNA. While some force fields show an erratic behavior when it comes to the reproduction of the higher-order DNA conformer space, OPLS and MMFF implementations are able to reproduce the experimentally known energy order. The stabilizing effect of the AA (anti−anti) versus SA (syn−anti) conformer is analyzed applying mechanical bond strength descriptors (compliance constants). The fact that we observe the correct energy order using appropriate force fields is in contrast with results previously reported, which suggested the general inappropriateness o…

OPLSMechanical bondChemistrycomputer.software_genreElectrostaticsForce field (chemistry)Computer Science Applicationschemistry.chemical_compoundClassical mechanicsSettore CHIM/03 - Chimica Generale E InorganicaDFT calculations Molecular mechanics calculations G-quadruplex DNADensity functional theoryData miningPhysical and Theoretical ChemistryGuanine-QuadruplexescomputerConformational isomerismDNAJournal of Chemical Theory and Computation
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