Enzymatic Methods for the Site-Specific Radiolabeling of Targeting Proteins |
| |
Authors: | Cristina Bolzati Barbara Spolaore |
| |
Institution: | 1.Institute of Condensed Matter Chemistry and Technologies for Energy ICMATE-CNR, Corso Stati Uniti, 4, I-35127 Padova, Italy;2.Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Via Marzolo, 5, I-35131 Padova, Italy;3.CRIBI Biotechnology Center, University of Padua, Viale G. Colombo, 3, I-35131 Padova, Italy |
| |
Abstract: | Site-specific conjugation of proteins is currently required to produce homogenous derivatives for medicine applications. Proteins derivatized at specific positions of the polypeptide chain can actually show higher stability, superior pharmacokinetics, and activity in vivo, as compared with conjugates modified at heterogeneous sites. Moreover, they can be better characterized regarding the composition of the derivatization sites as well as the conformational and activity properties. To this aim, several site-specific derivatization approaches have been developed. Among these, enzymes are powerful tools that efficiently allow the generation of homogenous protein–drug conjugates under physiological conditions, thus preserving their native structure and activity. This review will summarize the progress made over the last decade on the use of enzymatic-based methodologies for the production of site-specific labeled immunoconjugates of interest for nuclear medicine. Enzymes used in this field, including microbial transglutaminase, sortase, galactosyltransferase, and lipoic acid ligase, will be overviewed and their recent applications in the radiopharmaceutical field will be described. Since nuclear medicine can benefit greatly from the production of homogenous derivatives, we hope that this review will aid the use of enzymes for the development of better radio-conjugates for diagnostic and therapeutic purposes. |
| |
Keywords: | radioimmunoconjugates transglutaminase sortase lipoic acid ligase galactosyltransferase PET SPECT mAb nanobody affibody |
|
|