Challenges on Cyclic Nucleotide Phosphodiesterases Imaging with Positron Emission Tomography: Novel Radioligands and (Pre-)Clinical Insights since 2016.


Journal

International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791

Informations de publication

Date de publication:
07 Apr 2021
Historique:
received: 26 02 2021
revised: 29 03 2021
accepted: 31 03 2021
entrez: 30 4 2021
pubmed: 1 5 2021
medline: 21 5 2021
Statut: epublish

Résumé

Cyclic nucleotide phosphodiesterases (PDEs) represent one of the key targets in the research field of intracellular signaling related to the second messenger molecules cyclic adenosine monophosphate (cAMP) and/or cyclic guanosine monophosphate (cGMP). Hence, non-invasive imaging of this enzyme class by positron emission tomography (PET) using appropriate isoform-selective PDE radioligands is gaining importance. This methodology enables the in vivo diagnosis and staging of numerous diseases associated with altered PDE density or activity in the periphery and the central nervous system as well as the translational evaluation of novel PDE inhibitors as therapeutics. In this follow-up review, we summarize the efforts in the development of novel PDE radioligands and highlight (pre-)clinical insights from PET studies using already known PDE radioligands since 2016.

Identifiants

pubmed: 33917199
pii: ijms22083832
doi: 10.3390/ijms22083832
pmc: PMC8068090
pii:
doi:

Substances chimiques

Ligands 0
Radiopharmaceuticals 0
3',5'-Cyclic-AMP Phosphodiesterases EC 3.1.4.17
3',5'-Cyclic-GMP Phosphodiesterases EC 3.1.4.35

Types de publication

Journal Article Review

Langues

eng

Sous-ensembles de citation

IM

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Auteurs

Susann Schröder (S)

Department of Research and Development, ROTOP Pharmaka Ltd., 01328 Dresden, Germany.
Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Helmholtz-Zentrum Dresden-Rossendorf (HZDR), 04318 Leipzig, Germany.

Matthias Scheunemann (M)

Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Helmholtz-Zentrum Dresden-Rossendorf (HZDR), 04318 Leipzig, Germany.

Barbara Wenzel (B)

Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Helmholtz-Zentrum Dresden-Rossendorf (HZDR), 04318 Leipzig, Germany.

Peter Brust (P)

Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Helmholtz-Zentrum Dresden-Rossendorf (HZDR), 04318 Leipzig, Germany.

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Classifications MeSH