Sweetening Pharmaceutical Radiochemistry by ¹⁸F-Fluoroglycosylation: Recent Progress and Future Prospects

• Main Authors: Sandip S. Shinde (Author), Simone Maschauer (Author), Olaf Prante (Author)
• Format: Book
• Published: MDPI AG, 2021-11-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 10.3390/ph14111175; 1424-8247
• Keywords: fluorine-18; prosthetic group; ¹⁸F-fluoroglycosylation; positron emission tomography; PET; Medicine; R; Pharmacy and materia medica; RS1-441
• Source: Pharmaceuticals, Vol 14, Iss 11, p 1175 (2021)

In the field of ¹⁸F-chemistry for the development of radiopharmaceuticals for positron emission tomography (PET), various labeling strategies by the use of prosthetic groups have been implemented, including chemoselective ¹⁸F-labeling of biomolecules. Among those, chemoselective ¹⁸F-fluoroglycosylation methods focus on the sweetening of pharmaceutical radiochemistry by offering a highly valuable tool for the synthesis of ¹⁸F-glycoconjugates with suitable in vivo properties for PET imaging studies. A previous review covered the various ¹⁸F-fluoroglycosylation methods that were developed and applied as of 2014 (Maschauer and Prante, BioMed. Res. Int. 2014, 214748). This paper is an updated review, providing the recent progress in ¹⁸F-fluoroglycosylation reactions and the preclinical application of ¹⁸F-glycoconjugates, including small molecules, peptides, and high-molecular-weight proteins.