0000000000418857

AUTHOR

Francesco Papi

0000-0003-1760-1999

showing 2 related works from this author

Determinants for Tight and Selective Binding of a Medicinal Dicarbene Gold(I) Complex to a Telomeric DNA G-Quadruplex: a Joint ESI MS and XRD Investi…

2016

International audience; The dicarbene gold(I) complex [Au(9-methylcaffein-8-ylidene)(2)]BF4 is an exceptional organometallic compound of profound interest as a prospective anticancer agent. This gold(I) complex was previously reported to be highly cytotoxic toward various cancer cell lines invitro and behaves as a selective G-quadruplex stabilizer. Interactions of the gold complex with various telomeric DNA models have been analyzed by a combined ESI MS and X-ray diffraction (XRD) approach. ESI MS measurements confirmed formation of stable adducts between the intact gold(I) complex and Tel 23 DNA sequence. The crystal structure of the adduct formed between [Au(9-methylcaffein-8-ylidene)(2)]…

0301 basic medicineSpectrometry Mass Electrospray IonizationESI mass spectrometryStereochemistryElectrospray ionizationStackingESI mass spectrometry; G-quadruplexes; X-ray diffraction; cancer; gold[SDV.CAN]Life Sciences [q-bio]/CancerCrystal structurepotential anticancer agents010402 general chemistryG-quadruplex01 natural sciences[ CHIM ] Chemical SciencesCatalysisAdduct[ SDV.CAN ] Life Sciences [q-bio]/Cancerchemistry.chemical_compound03 medical and health sciencescancer[CHIM]Chemical SciencesChemistry010405 organic chemistryloop flexibilityapoptosiscrystal-structureGeneral ChemistryGeneral MedicineTelomeregoldG-quadruplexesinhibition3. Good health0104 chemical sciencesX-ray diffractionstabilizationcarbene complexessmall molecules030104 developmental biologypancreatic-cancer cellsX-ray crystallographySelectivityDNAmetal-complexes
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[Au(9-methylcaffein-8-ylidene) 2 ] + /DNA Tel23 System: Solution, Computational, and Biological Studies

2017

International audience; Physicochemical methods have been used to investigate interactions occurring in solution between the dicarbene gold(I) complex [Au(9‐methylcaffein‐8‐ylidene)2]BF4 (AuNHC) and a human telomeric DNA sequence, namely Tel23. Circular dichroism measurements allow identification of the conformational changes experienced by Tel23 upon interaction with AuNHC, and the respective binding stoichiometries and constants were determined. Computational studies provide a good link between previous crystallographic results of the same system and the present solution data, offering an exhaustive description of the inherent noncovalent metallodrug–DNA interactions. Remarkably, we found…

0301 basic medicineCircular dichroismSequence (biology)G-quadruplextelomerasehuman telomeric dnaCatalysisantitumor agentsk+ solutionAdductg-quadruplex structures03 medical and health sciencesMolecular dynamicschemistry.chemical_compoundanticancer agentsDNA structuresgold carbenes[CHIM]Chemical SciencesBinding sitechemistry.chemical_classificationcomplexesdensityligand-bindingChemistryOrganic Chemistrystructural basisGeneral ChemistrysequenceCombinatorial chemistryG-quadruplexescircular dichroismcircular-dichroism030104 developmental biologyEnzymeDNA
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