Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics
Autor(a) principal: | |
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Data de Publicação: | 2018 |
Outros Autores: | , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | http://hdl.handle.net/10316/107176 https://doi.org/10.3390/molecules24010049 |
Resumo: | Precision medicine relies on individually tailored therapeutic intervention taking into account individual variability. It is strongly dependent on the availability of target-specific drugs and/or imaging agents that recognize molecular targets and patient-specific disease mechanisms. The most sensitive molecular imaging modalities, Single Photon Emission Computed Tomography (SPECT) and Positron Emission Tomography (PET), rely on the interaction between an imaging radioprobe and a target. Moreover, the use of target-specific molecular tools for both diagnostics and therapy, theranostic agents, represent an established methodology in nuclear medicine that is assuming an increasingly important role in precision medicine. The design of innovative imaging and/or theranostic agents is key for further accomplishments in the field. G-protein-coupled receptors (GPCRs), apart from being highly relevant drug targets, have also been largely exploited as molecular targets for non-invasive imaging and/or systemic radiotherapy of various diseases. Herein, we will discuss recent efforts towards the development of innovative imaging and/or theranostic agents targeting selected emergent GPCRs, namely the Frizzled receptor (FZD), Ghrelin receptor (GHSR-1a), G protein-coupled estrogen receptor (GPER), and Sphingosine-1-phosphate receptor (S1PR). The pharmacological and clinical relevance will be highlighted, giving particular attention to the studies on the synthesis and characterization of targeted molecular imaging agents, biological evaluation, and potential clinical applications in oncology and non-oncology diseases. Whenever relevant, supporting computational studies will be also discussed. |
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Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranosticsfrizzled receptor (FZD)ghrelin receptor (GHSR-1a)G protein-coupled estrogen receptor (GPER)molecular imagingSphingosine-1-phosphate receptor (S1PR)theranosticsAnimalsDrug DiscoveryHumansReceptors, G-Protein-CoupledStructure-Activity RelationshipLigandsMolecular ImagingPrecision MedicineTheranostic NanomedicinePrecision medicine relies on individually tailored therapeutic intervention taking into account individual variability. It is strongly dependent on the availability of target-specific drugs and/or imaging agents that recognize molecular targets and patient-specific disease mechanisms. The most sensitive molecular imaging modalities, Single Photon Emission Computed Tomography (SPECT) and Positron Emission Tomography (PET), rely on the interaction between an imaging radioprobe and a target. Moreover, the use of target-specific molecular tools for both diagnostics and therapy, theranostic agents, represent an established methodology in nuclear medicine that is assuming an increasingly important role in precision medicine. The design of innovative imaging and/or theranostic agents is key for further accomplishments in the field. G-protein-coupled receptors (GPCRs), apart from being highly relevant drug targets, have also been largely exploited as molecular targets for non-invasive imaging and/or systemic radiotherapy of various diseases. Herein, we will discuss recent efforts towards the development of innovative imaging and/or theranostic agents targeting selected emergent GPCRs, namely the Frizzled receptor (FZD), Ghrelin receptor (GHSR-1a), G protein-coupled estrogen receptor (GPER), and Sphingosine-1-phosphate receptor (S1PR). The pharmacological and clinical relevance will be highlighted, giving particular attention to the studies on the synthesis and characterization of targeted molecular imaging agents, biological evaluation, and potential clinical applications in oncology and non-oncology diseases. Whenever relevant, supporting computational studies will be also discussed.MDPI2018-12-23info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://hdl.handle.net/10316/107176http://hdl.handle.net/10316/107176https://doi.org/10.3390/molecules24010049eng1420-3049Machado, João FrancoSilva, Rúben D.Melo, RitaCorreia, João D. G.info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2023-06-13T09:48:24Zoai:estudogeral.uc.pt:10316/107176Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T21:23:32.205558Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse |
dc.title.none.fl_str_mv |
Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics |
title |
Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics |
spellingShingle |
Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics Machado, João Franco frizzled receptor (FZD) ghrelin receptor (GHSR-1a) G protein-coupled estrogen receptor (GPER) molecular imaging Sphingosine-1-phosphate receptor (S1PR) theranostics Animals Drug Discovery Humans Receptors, G-Protein-Coupled Structure-Activity Relationship Ligands Molecular Imaging Precision Medicine Theranostic Nanomedicine |
title_short |
Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics |
title_full |
Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics |
title_fullStr |
Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics |
title_full_unstemmed |
Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics |
title_sort |
Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics |
author |
Machado, João Franco |
author_facet |
Machado, João Franco Silva, Rúben D. Melo, Rita Correia, João D. G. |
author_role |
author |
author2 |
Silva, Rúben D. Melo, Rita Correia, João D. G. |
author2_role |
author author author |
dc.contributor.author.fl_str_mv |
Machado, João Franco Silva, Rúben D. Melo, Rita Correia, João D. G. |
dc.subject.por.fl_str_mv |
frizzled receptor (FZD) ghrelin receptor (GHSR-1a) G protein-coupled estrogen receptor (GPER) molecular imaging Sphingosine-1-phosphate receptor (S1PR) theranostics Animals Drug Discovery Humans Receptors, G-Protein-Coupled Structure-Activity Relationship Ligands Molecular Imaging Precision Medicine Theranostic Nanomedicine |
topic |
frizzled receptor (FZD) ghrelin receptor (GHSR-1a) G protein-coupled estrogen receptor (GPER) molecular imaging Sphingosine-1-phosphate receptor (S1PR) theranostics Animals Drug Discovery Humans Receptors, G-Protein-Coupled Structure-Activity Relationship Ligands Molecular Imaging Precision Medicine Theranostic Nanomedicine |
description |
Precision medicine relies on individually tailored therapeutic intervention taking into account individual variability. It is strongly dependent on the availability of target-specific drugs and/or imaging agents that recognize molecular targets and patient-specific disease mechanisms. The most sensitive molecular imaging modalities, Single Photon Emission Computed Tomography (SPECT) and Positron Emission Tomography (PET), rely on the interaction between an imaging radioprobe and a target. Moreover, the use of target-specific molecular tools for both diagnostics and therapy, theranostic agents, represent an established methodology in nuclear medicine that is assuming an increasingly important role in precision medicine. The design of innovative imaging and/or theranostic agents is key for further accomplishments in the field. G-protein-coupled receptors (GPCRs), apart from being highly relevant drug targets, have also been largely exploited as molecular targets for non-invasive imaging and/or systemic radiotherapy of various diseases. Herein, we will discuss recent efforts towards the development of innovative imaging and/or theranostic agents targeting selected emergent GPCRs, namely the Frizzled receptor (FZD), Ghrelin receptor (GHSR-1a), G protein-coupled estrogen receptor (GPER), and Sphingosine-1-phosphate receptor (S1PR). The pharmacological and clinical relevance will be highlighted, giving particular attention to the studies on the synthesis and characterization of targeted molecular imaging agents, biological evaluation, and potential clinical applications in oncology and non-oncology diseases. Whenever relevant, supporting computational studies will be also discussed. |
publishDate |
2018 |
dc.date.none.fl_str_mv |
2018-12-23 |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://hdl.handle.net/10316/107176 http://hdl.handle.net/10316/107176 https://doi.org/10.3390/molecules24010049 |
url |
http://hdl.handle.net/10316/107176 https://doi.org/10.3390/molecules24010049 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
1420-3049 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.publisher.none.fl_str_mv |
MDPI |
publisher.none.fl_str_mv |
MDPI |
dc.source.none.fl_str_mv |
reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação instacron:RCAAP |
instname_str |
Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
instacron_str |
RCAAP |
institution |
RCAAP |
reponame_str |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
collection |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
repository.name.fl_str_mv |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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