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Does the Number of Bifunctional Chelators Conjugated to a mAb Affect the Biological Activity of Its Radio-Labeled Counterpart? Discussion Using the Example of mAb against CD-20 Labeled with (90)Y or (177)Lu

[Image: see text] There has been considerable interest in developing a monoclonal antibody (mAb) against-CD-20 (for example, Rituximab) modified by bifunctional chelating agents (BCA) for non-Hodgkin’s lymphoma radioimmunotherapy. Therefore, many researchers have modified this monoclonal antibody by...

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Autores principales: Karczmarczyk, Urszula, Sawicka, Agnieszka, Garnuszek, Piotr, Maurin, Michał, Wojdowska, Wioletta
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9109692/
https://www.ncbi.nlm.nih.gov/pubmed/35442675
http://dx.doi.org/10.1021/acs.jmedchem.1c02044
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author Karczmarczyk, Urszula
Sawicka, Agnieszka
Garnuszek, Piotr
Maurin, Michał
Wojdowska, Wioletta
author_facet Karczmarczyk, Urszula
Sawicka, Agnieszka
Garnuszek, Piotr
Maurin, Michał
Wojdowska, Wioletta
author_sort Karczmarczyk, Urszula
collection PubMed
description [Image: see text] There has been considerable interest in developing a monoclonal antibody (mAb) against-CD-20 (for example, Rituximab) modified by bifunctional chelating agents (BCA) for non-Hodgkin’s lymphoma radioimmunotherapy. Therefore, many researchers have modified this monoclonal antibody by attaching different BCA moieties and evaluated their biological activities in terms of in vitro study and in vivo study in healthy and tumor xenografted rodents. This mini-perspective reviews the in vitro studies, the immunoreactivity and physiological distribution studies: organ-to-blood and the tumor-to-organ ratio of conjugates with different numbers of chelators per mAb. We set up a null hypothesis that states there is no statistical significance between the biological activity of monoclonal antibody (Rituximab) and the number of conjugated bifunctional chelators. Overall, we have concluded that there is no strong evidence for this hypothesis. However, the literature data should be questioned due to the potential lack of uniform study methodology.
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spelling pubmed-91096922023-04-20 Does the Number of Bifunctional Chelators Conjugated to a mAb Affect the Biological Activity of Its Radio-Labeled Counterpart? Discussion Using the Example of mAb against CD-20 Labeled with (90)Y or (177)Lu Karczmarczyk, Urszula Sawicka, Agnieszka Garnuszek, Piotr Maurin, Michał Wojdowska, Wioletta J Med Chem [Image: see text] There has been considerable interest in developing a monoclonal antibody (mAb) against-CD-20 (for example, Rituximab) modified by bifunctional chelating agents (BCA) for non-Hodgkin’s lymphoma radioimmunotherapy. Therefore, many researchers have modified this monoclonal antibody by attaching different BCA moieties and evaluated their biological activities in terms of in vitro study and in vivo study in healthy and tumor xenografted rodents. This mini-perspective reviews the in vitro studies, the immunoreactivity and physiological distribution studies: organ-to-blood and the tumor-to-organ ratio of conjugates with different numbers of chelators per mAb. We set up a null hypothesis that states there is no statistical significance between the biological activity of monoclonal antibody (Rituximab) and the number of conjugated bifunctional chelators. Overall, we have concluded that there is no strong evidence for this hypothesis. However, the literature data should be questioned due to the potential lack of uniform study methodology. American Chemical Society 2022-04-20 2022-05-12 /pmc/articles/PMC9109692/ /pubmed/35442675 http://dx.doi.org/10.1021/acs.jmedchem.1c02044 Text en © 2022 The Authors. Published by American Chemical Society https://creativecommons.org/licenses/by-nc-nd/4.0/Permits non-commercial access and re-use, provided that author attribution and integrity are maintained; but does not permit creation of adaptations or other derivative works (https://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Karczmarczyk, Urszula
Sawicka, Agnieszka
Garnuszek, Piotr
Maurin, Michał
Wojdowska, Wioletta
Does the Number of Bifunctional Chelators Conjugated to a mAb Affect the Biological Activity of Its Radio-Labeled Counterpart? Discussion Using the Example of mAb against CD-20 Labeled with (90)Y or (177)Lu
title Does the Number of Bifunctional Chelators Conjugated to a mAb Affect the Biological Activity of Its Radio-Labeled Counterpart? Discussion Using the Example of mAb against CD-20 Labeled with (90)Y or (177)Lu
title_full Does the Number of Bifunctional Chelators Conjugated to a mAb Affect the Biological Activity of Its Radio-Labeled Counterpart? Discussion Using the Example of mAb against CD-20 Labeled with (90)Y or (177)Lu
title_fullStr Does the Number of Bifunctional Chelators Conjugated to a mAb Affect the Biological Activity of Its Radio-Labeled Counterpart? Discussion Using the Example of mAb against CD-20 Labeled with (90)Y or (177)Lu
title_full_unstemmed Does the Number of Bifunctional Chelators Conjugated to a mAb Affect the Biological Activity of Its Radio-Labeled Counterpart? Discussion Using the Example of mAb against CD-20 Labeled with (90)Y or (177)Lu
title_short Does the Number of Bifunctional Chelators Conjugated to a mAb Affect the Biological Activity of Its Radio-Labeled Counterpart? Discussion Using the Example of mAb against CD-20 Labeled with (90)Y or (177)Lu
title_sort does the number of bifunctional chelators conjugated to a mab affect the biological activity of its radio-labeled counterpart? discussion using the example of mab against cd-20 labeled with (90)y or (177)lu
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9109692/
https://www.ncbi.nlm.nih.gov/pubmed/35442675
http://dx.doi.org/10.1021/acs.jmedchem.1c02044
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