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https://observatorio.fm.usp.br/handle/OPI/28074
Title: | Synthesis of hydrophilic HYNIC-[1,2,4,5]tetrazine conjugates and their use in antibody pretargeting with Tc-99m |
Authors: | GARCIA, Maria Fernanda; GALLAZZI, Fabio; JUNQUEIRA, Mara de Souza; FERNANDEZ, Marcelo; CAMACHO, Ximena; MORORO, Janio da Silva; FARIA, Daniele; CARNEIRO, Camila de Godoi; COUTO, Marcos; CARRION, Federico; PRITSCH, Otto; CHAMMAS, Roger; QUINN, Thomas; CABRAL, Pablo; CERECETTO, Hugo |
Citation: | ORGANIC & BIOMOLECULAR CHEMISTRY, v.16, n.29, p.5275-5285, 2018 |
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. |
Appears in Collections: | Artigos e Materiais de Revistas Científicas - FM/MDR Artigos e Materiais de Revistas Científicas - HC/ICESP Artigos e Materiais de Revistas Científicas - LIM/21 Artigos e Materiais de Revistas Científicas - LIM/24 Artigos e Materiais de Revistas Científicas - LIM/43 |
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