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Issue 29, 2018
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Synthesis of hydrophilic HYNIC-[1,2,4,5]tetrazine conjugates and their use in antibody pretargeting with 99mTc

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Abstract

Pretargeted imaging, based on the highly reactive process between [1,2,4,5]tetrazines with trans-cyclooctene (TCO), appears as an attractive strategy to overcome disadvantages associated with traditional radioimmunoconjugates. To be successful, the radiolabeled component should react in vivo with the conjugated antibody and the non reactive excess clear fast from the organism. Herein, we explore the in vivo effects of hydrophilic linker incorporation into [1,2,4,5]tetrazine systems bearing a 6-hydrazinonicotinyl (HYNIC) moiety for technetium-99m coordination. Incorporation of a polypeptide chain containing hydrophilic aminoacids, resulted in a derivative with renal clearance. Pretargeted bevacizumab imaging was used as proof of concept.

Graphical abstract: Synthesis of hydrophilic HYNIC-[1,2,4,5]tetrazine conjugates and their use in antibody pretargeting with 99mTc

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Publication details

The article was received on 28 May 2018, accepted on 28 Jun 2018 and first published on 28 Jun 2018


Article type: Paper
DOI: 10.1039/C8OB01255E
Citation: Org. Biomol. Chem., 2018,16, 5275-5285
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    Synthesis of hydrophilic HYNIC-[1,2,4,5]tetrazine conjugates and their use in antibody pretargeting with 99mTc

    M. F. García, F. Gallazzi, M. D. S. Junqueira, M. Fernández, X. Camacho, J. D. S. Mororó, D. Faria, C. D. G. Carneiro, M. Couto, F. Carrión, O. Pritsch, R. Chammas, T. Quinn, P. Cabral and H. Cerecetto, Org. Biomol. Chem., 2018, 16, 5275
    DOI: 10.1039/C8OB01255E

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