Header

UZH-Logo

Maintenance Infos

The impact of emerging bioconjugation chemistries on radiopharmaceuticals


Fay, Rachael; Holland, Jason P (2019). The impact of emerging bioconjugation chemistries on radiopharmaceuticals. Journal of Nuclear Medicine, 60(5):587-591.

Abstract

The use of radiolabeled antibodies, immunoglobulin fragments and other proteins are an increasingly important sector of research for diagnostic imaging and targeted radiotherapy in Nuclear Medicine. As with all radiopharmaceuticals, efficient radiochemistry is a prerequisite to clinical translation. For proteins, variations in the primary amino acid sequence, the secondary structures and tertiary folds, as well as differences in size, charge, polarity, lipophilicity, and the presence of post-translational modifications, add complexity to the system. The choice of radionuclide or chelate, and their impact on the thermodynamic, kinetic and metabolic stability of a radiotracer has attracted much attention but the chemistry by which the radionuclide is conjugated to the protein scaffold is of equal importance. Recently, a wealth of creative advances in protein ligation methods based on chemical, photochemical and enzyme-mediated processes have emerged. As radiochemists explore alternative bioconjugation strategies, this article considers their potential impact on radiotracer design.

Abstract

The use of radiolabeled antibodies, immunoglobulin fragments and other proteins are an increasingly important sector of research for diagnostic imaging and targeted radiotherapy in Nuclear Medicine. As with all radiopharmaceuticals, efficient radiochemistry is a prerequisite to clinical translation. For proteins, variations in the primary amino acid sequence, the secondary structures and tertiary folds, as well as differences in size, charge, polarity, lipophilicity, and the presence of post-translational modifications, add complexity to the system. The choice of radionuclide or chelate, and their impact on the thermodynamic, kinetic and metabolic stability of a radiotracer has attracted much attention but the chemistry by which the radionuclide is conjugated to the protein scaffold is of equal importance. Recently, a wealth of creative advances in protein ligation methods based on chemical, photochemical and enzyme-mediated processes have emerged. As radiochemists explore alternative bioconjugation strategies, this article considers their potential impact on radiotracer design.

Statistics

Citations

Altmetrics

Downloads

30 downloads since deposited on 25 Apr 2019
30 downloads since 12 months
Detailed statistics

Additional indexing

Item Type:Journal Article, refereed, original work
Communities & Collections:07 Faculty of Science > Department of Chemistry
Dewey Decimal Classification:540 Chemistry
Language:English
Date:1 May 2019
Deposited On:25 Apr 2019 11:44
Last Modified:02 May 2019 01:05
Publisher:Society of Nuclear Medicine
ISSN:0161-5505
OA Status:Green
Free access at:Publisher DOI. An embargo period may apply.
Publisher DOI:https://doi.org/10.2967/jnumed.118.220806
Project Information:
  • : FunderSNSF
  • : Grant IDPP00P2_163683
  • : Project TitleAdvanced radiochemical methods for multi-modal imaging with nanomedicines
  • : FunderKrebsliga
  • : Grant IDKLS-4257-08-2017
  • : Project Title
  • : FunderH2020
  • : Grant ID676904
  • : Project TitleDeveloping multi-modality nanomedicines for targeted annotation of oncogenic signaling pathways

Download

Download PDF  'The impact of emerging bioconjugation chemistries on radiopharmaceuticals'.
Preview
Content: Accepted Version
Filetype: PDF
Size: 2MB
View at publisher