Pretargeted imaging beyond the blood–brain barrier

Author:

Shalgunov Vladimir1ORCID,Lopes van den Broek Sara1ORCID,Vang Andersen Ida1ORCID,García Vázquez Rocío1,Raval Nakul Ravi23,Palner Mikael24ORCID,Mori Yuki4ORCID,Schäfer Gabriela5,Herrmann Barbara6,Mikula Hannes6ORCID,Beschorner Natalie4,Nedergaard Maiken4,Syvänen Stina7ORCID,Barz Matthias48,Moos Knudsen Gitte29,Battisti Umberto Maria1ORCID,Herth Matthias Manfred110ORCID

Affiliation:

1. Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark

2. Neurobiology Research Unit and Center for Integrated Molecular Brain Imaging, Rigshospitalet Copenhagen University Hospital, Blegdamsvej 9, DK-2100 Copenhagen, Denmark

3. Faculty of Health and Medical Sciences, University of Copenhagen, 2200 Copenhagen, Denmark

4. Center for Translational Neuromedicine, University of Copenhagen, Blegdamsvej 3B, DK-2200 Copenhagen, Denmark

5. Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333CC Leiden, The Netherlands

6. Institute of Applied Synthetic Chemistry, Technische Universitat Wien (TU Wien), Getreidemarkt 9, 1060 Vienna, Austria

7. Rudbeck Laboratory, Department of Public Health and Caring Sciences, Uppsala University, Dag Hammarskjölds Väg 20, 75185 Uppsala, Sweden

8. Department of Dermatology, University Medical Center of the Johannes Gutenberg University Mainz, Langenbeckstraße 1, 55131 Mainz, Germany

9. Department of Clinical Medicine, University of Copenhagen, Denmark

10. Department of Clinical Physiology, Nuclear Medicine & PET, Rigshospitalet Copenhagen University Hospital, Blegdamsvej 9, 2100 Copenhagen, Denmark

Abstract

By screening a library of 18F-labeled tetrazines, we identified tetrazines which showed high pretargeted PET imaging contrast beyond the blood–brain-barrier.

Funder

Horizon 2020 Framework Programme

Danmarks Frie Forskningsfond

Novo Nordisk Fonden

Lundbeckfonden

Innovationsfonden

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Reference65 articles.

1. P. E.Edem and E. J. L.Stéen , Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates , Elsevier , Copenhagen , 1st edn, 2018

2. J. L.Kristensen and M. M.Herth , Textbook of drug design and discovery , CRC press , London and New York , 5th edn, 2017

3. Positron Emission Tomography in CNS Drug Discovery and Drug Monitoring

4. Molecular Imaging with PET

5. The theranostic path to personalized nanomedicine

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