G-quadruplexes and their ligands

Bibliographic Details
Main Author: Santos, Tiago
Publication Date: 2021
Other Authors: Salgado, Gilmar F., Cabrita, Eurico J., Cruz, Carla
Format: Other
Language: eng
Source: Repositórios Científicos de Acesso Aberto de Portugal (RCAAP)
Download full: http://hdl.handle.net/10362/124890
Summary: Funding 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.
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spelling G-quadruplexes and their ligandsBiophysical methods to unravel g-quadruplex/ligand interactionsBiophysical methodsG-quadruplexLigandsMolecular interactionsMolecular MedicinePharmaceutical ScienceDrug DiscoveryFunding 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.Progress 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.UCIBIO - Applied Molecular Biosciences UnitDQ - Departamento de QuímicaRUNSantos, TiagoSalgado, Gilmar F.Cabrita, Eurico J.Cruz, Carla2021-09-21T02:07:44Z2021-08-052021-08-05T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/otherapplication/pdfhttp://hdl.handle.net/10362/124890eng1424-8247PURE: 33384894https://doi.org/10.3390/ph14080769info:eu-repo/semantics/openAccessreponame:Repositórios Científicos de Acesso Aberto de Portugal (RCAAP)instname:FCCN, serviços digitais da FCT – Fundação para a Ciência e a Tecnologiainstacron:RCAAP2024-05-22T17:56:14Zoai:run.unl.pt:10362/124890Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireinfo@rcaap.ptopendoar:https://opendoar.ac.uk/repository/71602025-05-28T17:27:28.446492Repositórios Científicos de Acesso Aberto de Portugal (RCAAP) - FCCN, serviços digitais da FCT – Fundação para a Ciência e a Tecnologiafalse
dc.title.none.fl_str_mv G-quadruplexes and their ligands
Biophysical methods to unravel g-quadruplex/ligand interactions
title G-quadruplexes and their ligands
spellingShingle G-quadruplexes and their ligands
Santos, Tiago
Biophysical methods
G-quadruplex
Ligands
Molecular interactions
Molecular Medicine
Pharmaceutical Science
Drug Discovery
title_short G-quadruplexes and their ligands
title_full G-quadruplexes and their ligands
title_fullStr G-quadruplexes and their ligands
title_full_unstemmed G-quadruplexes and their ligands
title_sort G-quadruplexes and their ligands
author Santos, Tiago
author_facet Santos, Tiago
Salgado, Gilmar F.
Cabrita, Eurico J.
Cruz, Carla
author_role author
author2 Salgado, Gilmar F.
Cabrita, Eurico J.
Cruz, Carla
author2_role author
author
author
dc.contributor.none.fl_str_mv UCIBIO - Applied Molecular Biosciences Unit
DQ - Departamento de Química
RUN
dc.contributor.author.fl_str_mv Santos, Tiago
Salgado, Gilmar F.
Cabrita, Eurico J.
Cruz, Carla
dc.subject.por.fl_str_mv Biophysical methods
G-quadruplex
Ligands
Molecular interactions
Molecular Medicine
Pharmaceutical Science
Drug Discovery
topic Biophysical methods
G-quadruplex
Ligands
Molecular interactions
Molecular Medicine
Pharmaceutical Science
Drug Discovery
description Funding 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.
publishDate 2021
dc.date.none.fl_str_mv 2021-09-21T02:07:44Z
2021-08-05
2021-08-05T00:00:00Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/other
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status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10362/124890
url http://hdl.handle.net/10362/124890
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 1424-8247
PURE: 33384894
https://doi.org/10.3390/ph14080769
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