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G-quadruplexes and their ligands

2021-08-05Recensão Acesso aberto
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dc.contributor.authorSantos, Tiago
dc.contributor.authorSalgado, Gilmar F.
dc.contributor.authorCabrita, Eurico J.
dc.contributor.authorCruz, Carla
dc.contributor.institutionUCIBIO - Applied Molecular Biosciences Unit
dc.contributor.institutionDQ - Departamento de Química
dc.contributor.pblMolecular Diversity Preservation International (MDPI)
dc.date.accessioned2021-09-21T02:07:44Z
dc.date.available2021-09-21T02:07:44Z
dc.date.issued2021-08-05
dc.descriptionFunding Information: (PD/00065/2013). This work was supported by PESSOA program ref. 5079 and project “Projeto de Investigação Exploratória” ref. IF/00959/2015 entitled “NCL targeting by G-quadruplex aptamers for cervical cancer therapy” financed by Fundo Social Europeu e Programa Operacional Potencial Humano. Thanks are due to FCT/MCT for the financial support of the CICS-UBI UIDB/00709/2020 research unit and to the Portuguese NMR Network (ROTEIRO/0031/2013-PINFRA/22161/2016), through national funds and, where applicable, supported by European Investment Funds FEDER through COMPETE 2020, POCI, PORL and PIDDAC.
dc.description.abstractProgress in the design of G-quadruplex (G4) binding ligands relies on the availability of approaches that assess the binding mode and nature of the interactions between G4 forming sequences and their putative ligands. The experimental approaches used to characterize G4/ligand interactions can be categorized into structure-based methods (circular dichroism (CD), nuclear magnetic resonance (NMR) spectroscopy and X-ray crystallography), affinity and apparent affinity-based methods (surface plasmon resonance (SPR), isothermal titration calorimetry (ITC) and mass spectrometry (MS)), and high-throughput methods (fluorescence resonance energy transfer (FRET)-melting, G4-fluorescent intercalator displacement assay (G4-FID), affinity chromatography and microarrays. Each method has unique advantages and drawbacks, which makes it essential to select the ideal strategies for the biological question being addressed. The structural-and affinity and apparent affinity-based methods are in several cases complex and/or time-consuming and can be combined with fast and cheap high-throughput approaches to improve the design and development of new potential G4 ligands. In recent years, the joint use of these techniques permitted the discovery of a huge number of G4 ligands investigated for diagnostic and therapeutic purposes. Overall, this review article highlights in detail the most commonly used approaches to characterize the G4/ligand interactions, as well as the applications and types of information that can be obtained from the use of each technique.en
dc.description.versionpublishersversion
dc.description.versionpublished
dc.format.extent9034776
dc.identifier.doi10.3390/ph14080769
dc.identifier.issn1424-8247
dc.identifier.otherPURE: 33384894
dc.identifier.otherPURE UUID: 2282b77b-9a73-42f5-b285-c5a815458a9e
dc.identifier.otherScopus: 85112480328
dc.identifier.otherPubMed: 34451866
dc.identifier.otherPubMedCentral: PMC8401999
dc.identifier.otherWOS: 000689782500001
dc.identifier.urihttp://hdl.handle.net/10362/124890
dc.identifier.urlhttps://www.scopus.com/pages/publications/85112480328
dc.language.isoeng
dc.peerreviewedyes
dc.relationinfo:eu-repo/grantAgreement/FCT/POR_CENTRO/PD%2FBD%2F142851%2F2018/PT
dc.relationStructural determination of pre-miR 149 - G4 ligand - Nucleolin complex
dc.relationNucleolin targeting by G-quadruplex aptamers for cervical cancer therapy
dc.subjectBiophysical methods
dc.subjectG-quadruplex
dc.subjectLigands
dc.subjectMolecular interactions
dc.subjectMolecular Medicine
dc.subjectPharmaceutical Science
dc.subjectDrug Discovery
dc.titleG-quadruplexes and their ligandsen
dc.title.subtitleBiophysical methods to unravel g-quadruplex/ligand interactionsen
dc.typereview
degois.publication.issue8
degois.publication.titlePharmaceuticals
degois.publication.volume14
dspace.entity.typePublication
oaire.awardNumberPD/BD/142851/2018
oaire.awardNumberIF/00959/2015/CP1300/CT0002
oaire.awardTitleStructural determination of pre-miR 149 - G4 ligand - Nucleolin complex
oaire.awardTitleNucleolin targeting by G-quadruplex aptamers for cervical cancer therapy
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/POR_CENTRO/PD%2FBD%2F142851%2F2018/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/Investigador FCT/IF%2F00959%2F2015%2FCP1300%2FCT0002/PT
oaire.fundingStreamPOR_CENTRO
oaire.fundingStreamInvestigador FCT
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsopenAccess
relation.isProjectOfPublicationd2941657-70ba-414c-b453-b16a82b14c72
relation.isProjectOfPublication7633edcf-54d2-47b5-a47a-6c31cbbb0220
relation.isProjectOfPublication.latestForDiscovery7633edcf-54d2-47b5-a47a-6c31cbbb0220

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