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Development of the ...
Development of the First Tritiated Tetrazine : Facilitating Tritiation of Proteins
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- Bidesi, Natasha Shalina Radjani (författare)
- Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, Jagtvej 160, DK-2100 Copenhagen, Denmark.
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- Battisti, Umberto Maria (författare)
- Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, Jagtvej 160, DK-2100 Copenhagen, Denmark.
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- van de Broek, Sara Lopes (författare)
- Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, Jagtvej 160, DK-2100 Copenhagen, Denmark.
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- Shalgunov, Vladimir (författare)
- Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, Jagtvej 160, DK-2100 Copenhagen, Denmark.;Rigshosp, Dept Clin Physiol, Nucl Med, Blegdamsvej 9, DK-2100 Copenhagen, Denmark.;Rigshosp, PET, Blegdamsvej 9, DK-2100 Copenhagen, Denmark.
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- Dall, Anne-Mette (författare)
- Novo Nordisk AS, Smormosevej 17-19, DK-2880 Copenhagen, Denmark.
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- Kristensen, Jesper Boggild (författare)
- Novo Nordisk AS, Smormosevej 17-19, DK-2880 Copenhagen, Denmark.
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- Sehlin, Dag, 1976- (författare)
- Uppsala universitet,Institutionen för folkhälso- och vårdvetenskap
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- Syvänen, Stina (författare)
- Uppsala universitet,Institutionen för folkhälso- och vårdvetenskap
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- Knudsen, Gitte Moos (författare)
- Rigshosp, Neurobiol Res Unit, Blegdamsvej 9, DK-2100 Copenhagen, Denmark.
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- Herth, Matthias Manfred (författare)
- Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, Jagtvej 160, DK-2100 Copenhagen, Denmark.;Rigshosp, Dept Clin Physiol, Nucl Med, Blegdamsvej 9, DK-2100 Copenhagen, Denmark.;Rigshosp, PET, Blegdamsvej 9, DK-2100 Copenhagen, Denmark.
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Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, Jagtvej 160, DK-2100 Copenhagen, Denmark Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, Jagtvej 160, DK-2100 Copenhagen, Denmark.;Rigshosp, Dept Clin Physiol, Nucl Med, Blegdamsvej 9, DK-2100 Copenhagen, Denmark.;Rigshosp, PET, Blegdamsvej 9, DK-2100 Copenhagen, Denmark. (creator_code:org_t)
- 2022-11-04
- 2022
- Engelska.
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Ingår i: ChemBioChem. - : John Wiley & Sons. - 1439-4227 .- 1439-7633. ; 23:23
- Relaterad länk:
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https://doi.org/10.1...
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https://uu.diva-port... (primary) (Raw object)
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- Tetrazine (Tz)-trans-cyclooctene (TCO) ligation is an ultra-fast and highly selective reaction and it is particularly suited to label biomolecules under physiological conditions. As such, a H-3-Tz based synthon would have wide applications for in vitro/ex vivo assays. In this study, we developed a H-3-labeled Tz and characterized its potential for application to pretargeted autoradiography. Several strategies were explored to synthesize such a Tz. However, classical approaches such as reductive halogenation failed. For this reason, we designed a Tz containing an aldehyde and explored the possibility of reducing this group with NaBT4. This approach was successful and resulted in [H-3]-(4-(6-(pyridin-2-yl)-1,2,4,5-tetrazin-3-yl)phenyl)methan-t-ol with a radiochemical yield of 22 %, a radiochemical purity of 96 % and a molar activity of 0.437 GBq/mu mol (11.8 Ci/mmol). The compound was successfully applied to pretargeted autoradiography. Thus, we report the synthesis of the first H-3-labeled Tz and its successful application as a labeling building block.
Ämnesord
- NATURVETENSKAP -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
Nyckelord
- autoradiography
- bioorthogonal chemistry
- pre-targeting
- tetrazine ligation
- tritiation
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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Bidesi, Natasha ...
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Battisti, Umbert ...
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van de Broek, Sa ...
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Shalgunov, Vladi ...
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Dall, Anne-Mette
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Kristensen, Jesp ...
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Sehlin, Dag, 197 ...
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Syvänen, Stina
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Knudsen, Gitte M ...
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Herth, Matthias ...
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- NATURVETENSKAP
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NATURVETENSKAP
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och Biologi
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och Biokemi och mole ...
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ChemBioChem
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Uppsala universitet