PT  - JOURNAL ARTICLE
AU  - Rachael Fay
AU  - Jason P. Holland
TI  - The impact of emerging bioconjugation chemistries on radiopharmaceuticals
AID  - 10.2967/jnumed.118.220806
DP  - 2019 Mar 01
TA  - Journal of Nuclear Medicine
PG  - jnumed.118.220806
4099  - http://jnm.snmjournals.org/content/early/2019/03/21/jnumed.118.220806.short
4100  - http://jnm.snmjournals.org/content/early/2019/03/21/jnumed.118.220806.full
AB  - 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.