<div class="csl-bib-body">
<div class="csl-entry">Battisti, U. M., Bratteby, K., Jørgensen, J. T., Hvass, L., Shalgunov, V., Mikula, H., Kjær, A., & Herth, M. M. (2021). Development of the First Aliphatic <sup>1</sup><sup>8</sup>F-Labeled Tetrazine Suitable for Pretargeted PET Imaging-Expanding the Bioorthogonal Tool Box. <i>Journal of Medicinal Chemistry</i>, <i>64</i>(20), 15297–15312. https://doi.org/10.1021/acs.jmedchem.1c01326</div>
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dc.identifier.issn
0022-2623
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dc.identifier.uri
http://hdl.handle.net/20.500.12708/138462
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dc.description.abstract
Pretargeted imaging of nanomedicines have attracted considerable interest because it has the potential to increase imaging contrast while reducing radiation burden to healthy tissue. Currently, the tetrazine ligation is the fastest bioorthogonal reaction for this strategy and, consequently, the state-of-art choice for in vivo chemistry. We have recently identified key properties for tetrazines in pretargeting. We have also developed a method to 18F-label reactive tetrazines using an aliphatic nucleophilic substitution strategy. Here, we combined this knowledge and developed an 18F-labeled tetrazine for pretargeted imaging. In order to develop this ligand, a small SAR study was performed. The most promising compound was selected for labeling and subsequent positron-emission-tomography in vivo imaging. Radiolabeling was achieved in satisfactory yields, molar activities, and high radiochemical purities. [18F]15 displayed favorable pharmacokinetics and remarkable target-to-background ratios-as early as 1 h post injection. We believe that this agent could be a promising candidate for translation into clinical studies.
en
dc.language.iso
en
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dc.publisher
AMER CHEMICAL SOC
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dc.relation.ispartof
Journal of Medicinal Chemistry
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dc.subject
Click Chemistry
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dc.subject
Drug Discovery
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dc.subject
Molecular Medicine
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dc.subject
synthetic chemistry
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dc.title
Development of the First Aliphatic ¹⁸F-Labeled Tetrazine Suitable for Pretargeted PET Imaging-Expanding the Bioorthogonal Tool Box
en
dc.type
Artikel
de
dc.type
Article
en
dc.description.startpage
15297
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dc.description.endpage
15312
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dc.type.category
Original Research Article
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tuw.container.volume
64
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tuw.container.issue
20
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tuw.journal.peerreviewed
true
-
tuw.peerreviewed
true
-
wb.publication.intCoWork
International Co-publication
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tuw.researchTopic.id
X1
-
tuw.researchTopic.name
außerhalb der gesamtuniversitären Forschungsschwerpunkte
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tuw.researchTopic.value
100
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dcterms.isPartOf.title
Journal of Medicinal Chemistry
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tuw.publication.orgunit
E163-03-2 - Forschungsgruppe Molekulare Chemie und Chemische Biologie
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tuw.publisher.doi
10.1021/acs.jmedchem.1c01326
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dc.identifier.eissn
1520-4804
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dc.description.numberOfPages
16
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tuw.author.orcid
0000-0003-0930-2390
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tuw.author.orcid
0000-0002-9218-9722
-
tuw.author.orcid
0000-0002-2706-5547
-
tuw.author.orcid
0000-0002-7788-513X
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wb.sci
true
-
wb.sciencebranch
Chemie
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wb.sciencebranch
Pharmazie, Pharmakologie, Toxikologie
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wb.sciencebranch.oefos
1040
-
wb.sciencebranch.oefos
3012
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wb.facultyfocus
Chemistry and Technology of Materials
de
wb.facultyfocus
Chemistry and Technology of Materials
en
wb.facultyfocus.faculty
E150
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item.languageiso639-1
en
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item.fulltext
no Fulltext
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item.openairetype
research article
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item.cerifentitytype
Publications
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item.openairecristype
http://purl.org/coar/resource_type/c_2df8fbb1
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item.grantfulltext
restricted
-
crisitem.author.dept
E163-03-2 - Forschungsgruppe Molekulare Chemie und Chemische Biologie
-
crisitem.author.orcid
0000-0002-9218-9722
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crisitem.author.parentorg
E163-03 - Forschungsbereich Organische und Biologische Chemie