Novel Radioligands for Cyclic Nucleotide Phosphodiesterase Imaging with Positron Emission Tomography: An Update on Developments Since 2012
Cyclic nucleotide phosphodiesterases (PDEs) are a class of intracellular enzymes that inactivate the secondary messenger molecules, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). Thus, PDEs regulate the signaling cascades mediated by these cyclic nucleotides and aff...
Main Authors: | , , , , |
---|---|
Format: | Article |
Language: | English |
Published: |
MDPI AG
2016-05-01
|
Series: | Molecules |
Subjects: | |
Online Access: | http://www.mdpi.com/1420-3049/21/5/650 |
_version_ | 1829500332367937536 |
---|---|
author | Susann Schröder Barbara Wenzel Winnie Deuther-Conrad Matthias Scheunemann Peter Brust |
author_facet | Susann Schröder Barbara Wenzel Winnie Deuther-Conrad Matthias Scheunemann Peter Brust |
author_sort | Susann Schröder |
collection | DOAJ |
description | Cyclic nucleotide phosphodiesterases (PDEs) are a class of intracellular enzymes that inactivate the secondary messenger molecules, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). Thus, PDEs regulate the signaling cascades mediated by these cyclic nucleotides and affect fundamental intracellular processes. Pharmacological inhibition of PDE activity is a promising strategy for treatment of several diseases. However, the role of the different PDEs in related pathologies is not completely clarified yet. PDE-specific radioligands enable non-invasive visualization and quantification of these enzymes by positron emission tomography (PET) in vivo and provide an important translational tool for elucidation of the relationship between altered expression of PDEs and pathophysiological effects as well as (pre-)clinical evaluation of novel PDE inhibitors developed as therapeutics. Herein we present an overview of novel PDE radioligands for PET published since 2012. |
first_indexed | 2024-12-16T08:54:05Z |
format | Article |
id | doaj.art-080b80bcecf243f8bfa85a8ad9faca6a |
institution | Directory Open Access Journal |
issn | 1420-3049 |
language | English |
last_indexed | 2024-12-16T08:54:05Z |
publishDate | 2016-05-01 |
publisher | MDPI AG |
record_format | Article |
series | Molecules |
spelling | doaj.art-080b80bcecf243f8bfa85a8ad9faca6a2022-12-21T22:37:20ZengMDPI AGMolecules1420-30492016-05-0121565010.3390/molecules21050650molecules21050650Novel Radioligands for Cyclic Nucleotide Phosphodiesterase Imaging with Positron Emission Tomography: An Update on Developments Since 2012Susann Schröder0Barbara Wenzel1Winnie Deuther-Conrad2Matthias Scheunemann3Peter Brust4Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf, Permoserstraße 15, Leipzig 04318, GermanyDepartment of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf, Permoserstraße 15, Leipzig 04318, GermanyDepartment of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf, Permoserstraße 15, Leipzig 04318, GermanyDepartment of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf, Permoserstraße 15, Leipzig 04318, GermanyDepartment of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf, Permoserstraße 15, Leipzig 04318, GermanyCyclic nucleotide phosphodiesterases (PDEs) are a class of intracellular enzymes that inactivate the secondary messenger molecules, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). Thus, PDEs regulate the signaling cascades mediated by these cyclic nucleotides and affect fundamental intracellular processes. Pharmacological inhibition of PDE activity is a promising strategy for treatment of several diseases. However, the role of the different PDEs in related pathologies is not completely clarified yet. PDE-specific radioligands enable non-invasive visualization and quantification of these enzymes by positron emission tomography (PET) in vivo and provide an important translational tool for elucidation of the relationship between altered expression of PDEs and pathophysiological effects as well as (pre-)clinical evaluation of novel PDE inhibitors developed as therapeutics. Herein we present an overview of novel PDE radioligands for PET published since 2012.http://www.mdpi.com/1420-3049/21/5/650positron emission tomographyphosphodiesterasescyclic nucleotide signalingPDE inhibitorsPDE radioligandsimaging |
spellingShingle | Susann Schröder Barbara Wenzel Winnie Deuther-Conrad Matthias Scheunemann Peter Brust Novel Radioligands for Cyclic Nucleotide Phosphodiesterase Imaging with Positron Emission Tomography: An Update on Developments Since 2012 Molecules positron emission tomography phosphodiesterases cyclic nucleotide signaling PDE inhibitors PDE radioligands imaging |
title | Novel Radioligands for Cyclic Nucleotide Phosphodiesterase Imaging with Positron Emission Tomography: An Update on Developments Since 2012 |
title_full | Novel Radioligands for Cyclic Nucleotide Phosphodiesterase Imaging with Positron Emission Tomography: An Update on Developments Since 2012 |
title_fullStr | Novel Radioligands for Cyclic Nucleotide Phosphodiesterase Imaging with Positron Emission Tomography: An Update on Developments Since 2012 |
title_full_unstemmed | Novel Radioligands for Cyclic Nucleotide Phosphodiesterase Imaging with Positron Emission Tomography: An Update on Developments Since 2012 |
title_short | Novel Radioligands for Cyclic Nucleotide Phosphodiesterase Imaging with Positron Emission Tomography: An Update on Developments Since 2012 |
title_sort | novel radioligands for cyclic nucleotide phosphodiesterase imaging with positron emission tomography an update on developments since 2012 |
topic | positron emission tomography phosphodiesterases cyclic nucleotide signaling PDE inhibitors PDE radioligands imaging |
url | http://www.mdpi.com/1420-3049/21/5/650 |
work_keys_str_mv | AT susannschroder novelradioligandsforcyclicnucleotidephosphodiesteraseimagingwithpositronemissiontomographyanupdateondevelopmentssince2012 AT barbarawenzel novelradioligandsforcyclicnucleotidephosphodiesteraseimagingwithpositronemissiontomographyanupdateondevelopmentssince2012 AT winniedeutherconrad novelradioligandsforcyclicnucleotidephosphodiesteraseimagingwithpositronemissiontomographyanupdateondevelopmentssince2012 AT matthiasscheunemann novelradioligandsforcyclicnucleotidephosphodiesteraseimagingwithpositronemissiontomographyanupdateondevelopmentssince2012 AT peterbrust novelradioligandsforcyclicnucleotidephosphodiesteraseimagingwithpositronemissiontomographyanupdateondevelopmentssince2012 |