Farleigh, M;
Pham, TT;
Yu, Z;
Kim, J;
Sunassee, K;
Firth, G;
Forte, N;
... Ma, MT; + view all
(2021)
New Bifunctional Chelators Incorporating Dibromomaleimide Groups for Radiolabeling of Antibodies with Positron Emission Tomography Imaging Radioisotopes.
Bioconjugate Chemistry
, 32
(7)
pp. 1214-1222.
10.1021/acs.bioconjchem.0c00710.
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Abstract
Positron Emission Tomography (PET) imaging with antibody-based contrast agents frequently uses the radioisotopes [{64}^Cu]Cu^{2+} and [{89}^Zr]Zr^{4+}. The macrobicyclic chelator commonly known as sarcophagine (sar) is ideal for labeling receptor-targeted biomolecules with [{64}^Cu]Cu^{2+}. The siderophore chelator, desferrioxamine-B (dfo), has been widely used to incorporate [{89}^Zr]Zr^{4+}, respectively, in near quantitative radiochemical yield (>99%). Serum stability studies, in vivo PET imaging, and biodistribution analyses using these radiolabeled immunoconjugates demonstrate that both [{64}^Cu]Cu-sar–dtm–trastuzumab and [{89}^Zr]Zr-dfo–dtm–trastuzumab possess high stability in biological milieu. Dibromomaleimide technology can be easily applied to enable stable, site-specific attachment of radiolabeled chelators, such as sar and dfo, to native interstrand disulfide regions of antibodies, enabling tracking of antibodies with PET imaging.
| Type: | Article |
|---|---|
| Title: | New Bifunctional Chelators Incorporating Dibromomaleimide Groups for Radiolabeling of Antibodies with Positron Emission Tomography Imaging Radioisotopes |
| Location: | United States |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1021/acs.bioconjchem.0c00710 |
| Publisher version: | https://doi.org/10.1021/acs.bioconjchem.0c00710 |
| Language: | English |
| Additional information: | This version is the author accepted manuscript. For information on re-use, please refer to the publisher's terms and conditions. |
| Keywords: | Biopolymers, Conjugate acid-base pairs, Immunology, Mechanisms of action, Peptides and proteins |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > UCL BEAMS UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences > Dept of Chemistry |
| URI: | https://discovery.ucl.ac.uk/id/eprint/10126047 |
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