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Novel Radioligands for Cyclic Nucleotide Phosphodiesterase Imaging with Positron Emission Tomography: An Update on Developments Since 2012. | LitMetric

AI Article Synopsis

  • PDEs are enzymes that deactivate key signaling molecules (cAMP and cGMP), influencing crucial intracellular processes and pathways.
  • Inhibiting PDE activity shows potential for treating various diseases, though the specific roles of different PDEs in these conditions are still under investigation.
  • Novel PDE-specific radioligands developed for PET imaging allow for non-invasive monitoring of these enzymes, aiding in understanding their involvement in diseases and evaluating new treatments.

Article Abstract

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.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273803PMC
http://dx.doi.org/10.3390/molecules21050650DOI Listing

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