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Radiolabeling Strategies for Tumor-Targeting Proteinaceous Drugs

Owing to their large size proteinaceous drugs offer higher operative information content compared to the small molecules that correspond to the traditional understanding of druglikeness. As a consequence these drugs allow developing patient-specific therapies that provide the means to go beyond the...

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Autores principales: Sugiura, Grant, Kühn, Helen, Sauter, Max, Haberkorn, Uwe, Mier, Walter
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271853/
https://www.ncbi.nlm.nih.gov/pubmed/24552984
http://dx.doi.org/10.3390/molecules19022135
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author Sugiura, Grant
Kühn, Helen
Sauter, Max
Haberkorn, Uwe
Mier, Walter
author_facet Sugiura, Grant
Kühn, Helen
Sauter, Max
Haberkorn, Uwe
Mier, Walter
author_sort Sugiura, Grant
collection PubMed
description Owing to their large size proteinaceous drugs offer higher operative information content compared to the small molecules that correspond to the traditional understanding of druglikeness. As a consequence these drugs allow developing patient-specific therapies that provide the means to go beyond the possibilities of current drug therapy. However, the efficacy of these strategies, in particular “personalized medicine”, depends on precise information about individual target expression rates. Molecular imaging combines non-invasive imaging methods with tools of molecular and cellular biology and thus bridges current knowledge to the clinical use. Moreover, nuclear medicine techniques provide therapeutic applications with tracers that behave like the diagnostic tracer. The advantages of radioiodination, still the most versatile radiolabeling strategy, and other labeled compounds comprising covalently attached radioisotopes are compared to the use of chelator-protein conjugates that are complexed with metallic radioisotopes. With the techniques using radioactive isotopes as a reporting unit or even the therapeutic principle, care has to be taken to avoid cleavage of the radionuclide from the protein it is linked to. The tracers used in molecular imaging require labeling techniques that provide site specific conjugation and metabolic stability. Appropriate choice of the radionuclide allows tailoring the properties of the labeled protein to the application required. Until the event of positron emission tomography the spectrum of nuclides used to visualize cellular and biochemical processes was largely restricted to iodine isotopes and 99m-technetium. Today, several nuclides such as 18-fluorine, 68-gallium and 86-yttrium have fundamentally extended the possibilities of tracer design and in turn caused the need for the development of chemical methods for their conjugation.
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spelling pubmed-62718532018-12-20 Radiolabeling Strategies for Tumor-Targeting Proteinaceous Drugs Sugiura, Grant Kühn, Helen Sauter, Max Haberkorn, Uwe Mier, Walter Molecules Review Owing to their large size proteinaceous drugs offer higher operative information content compared to the small molecules that correspond to the traditional understanding of druglikeness. As a consequence these drugs allow developing patient-specific therapies that provide the means to go beyond the possibilities of current drug therapy. However, the efficacy of these strategies, in particular “personalized medicine”, depends on precise information about individual target expression rates. Molecular imaging combines non-invasive imaging methods with tools of molecular and cellular biology and thus bridges current knowledge to the clinical use. Moreover, nuclear medicine techniques provide therapeutic applications with tracers that behave like the diagnostic tracer. The advantages of radioiodination, still the most versatile radiolabeling strategy, and other labeled compounds comprising covalently attached radioisotopes are compared to the use of chelator-protein conjugates that are complexed with metallic radioisotopes. With the techniques using radioactive isotopes as a reporting unit or even the therapeutic principle, care has to be taken to avoid cleavage of the radionuclide from the protein it is linked to. The tracers used in molecular imaging require labeling techniques that provide site specific conjugation and metabolic stability. Appropriate choice of the radionuclide allows tailoring the properties of the labeled protein to the application required. Until the event of positron emission tomography the spectrum of nuclides used to visualize cellular and biochemical processes was largely restricted to iodine isotopes and 99m-technetium. Today, several nuclides such as 18-fluorine, 68-gallium and 86-yttrium have fundamentally extended the possibilities of tracer design and in turn caused the need for the development of chemical methods for their conjugation. MDPI 2014-02-18 /pmc/articles/PMC6271853/ /pubmed/24552984 http://dx.doi.org/10.3390/molecules19022135 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Review
Sugiura, Grant
Kühn, Helen
Sauter, Max
Haberkorn, Uwe
Mier, Walter
Radiolabeling Strategies for Tumor-Targeting Proteinaceous Drugs
title Radiolabeling Strategies for Tumor-Targeting Proteinaceous Drugs
title_full Radiolabeling Strategies for Tumor-Targeting Proteinaceous Drugs
title_fullStr Radiolabeling Strategies for Tumor-Targeting Proteinaceous Drugs
title_full_unstemmed Radiolabeling Strategies for Tumor-Targeting Proteinaceous Drugs
title_short Radiolabeling Strategies for Tumor-Targeting Proteinaceous Drugs
title_sort radiolabeling strategies for tumor-targeting proteinaceous drugs
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271853/
https://www.ncbi.nlm.nih.gov/pubmed/24552984
http://dx.doi.org/10.3390/molecules19022135
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