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Molecules 2016, 21(5), 650; doi:10.3390/molecules21050650

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

Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf, Permoserstraße 15, Leipzig 04318, Germany
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Author to whom correspondence should be addressed.
Academic Editor: Zhen Cheng
Received: 14 April 2016 / Revised: 9 May 2016 / Accepted: 10 May 2016 / Published: 19 May 2016
(This article belongs to the Special Issue Molecular Imaging Probes)

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. View Full-Text
Keywords: positron emission tomography; phosphodiesterases; cyclic nucleotide signaling; PDE inhibitors; PDE radioligands; imaging positron emission tomography; phosphodiesterases; cyclic nucleotide signaling; PDE inhibitors; PDE radioligands; imaging
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Schröder, S.; Wenzel, B.; Deuther-Conrad, W.; Scheunemann, M.; Brust, P. Novel Radioligands for Cyclic Nucleotide Phosphodiesterase Imaging with Positron Emission Tomography: An Update on Developments Since 2012. Molecules 2016, 21, 650.

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