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Review

Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics

1
Centro de Ciências e Tecnologias Nucleares, Instituto Superior Técnico, Universidade de Lisboa, CTN, Estrada Nacional 10 (km 139,7), 2695-066 Bobadela LRS, Portugal
2
Centro de Química Estrutural, Faculdade de Ciências, Universidade de Lisboa, 1749-016 Lisboa, Portugal
3
Center for Neuroscience and Cell Biology; Rua Larga, Faculdade de Medicina, Polo I, 1ºandar, Universidade de Coimbra, 3004-504 Coimbra, Portugal
*
Author to whom correspondence should be addressed.
Academic Editor: Irina S. Moreira
Received: 18 November 2018 / Revised: 7 December 2018 / Accepted: 9 December 2018 / Published: 23 December 2018
(This article belongs to the Special Issue GPCR Mechanism and Drug Design)
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. View Full-Text
Keywords: frizzled receptor (FZD); ghrelin receptor (GHSR-1a); G protein-coupled estrogen receptor (GPER); molecular imaging; Sphingosine-1-phosphate receptor (S1PR); theranostics frizzled receptor (FZD); ghrelin receptor (GHSR-1a); G protein-coupled estrogen receptor (GPER); molecular imaging; Sphingosine-1-phosphate receptor (S1PR); theranostics
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MDPI and ACS Style

Franco Machado, J.; Silva, R.D.; Melo, R.; G. Correia, J.D. Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics. Molecules 2019, 24, 49. https://0-doi-org.brum.beds.ac.uk/10.3390/molecules24010049

AMA Style

Franco Machado J, Silva RD, Melo R, G. Correia JD. Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics. Molecules. 2019; 24(1):49. https://0-doi-org.brum.beds.ac.uk/10.3390/molecules24010049

Chicago/Turabian Style

Franco Machado, João, Rúben D. Silva, Rita Melo, and João D. G. Correia. 2019. "Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics" Molecules 24, no. 1: 49. https://0-doi-org.brum.beds.ac.uk/10.3390/molecules24010049

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