Synthesis, Fluorine-18 Radiolabeling, and In Vivo PET Imaging of a Hydrophilic Fluorosulfotetrazine

• Published in: Pharmaceuticals (Basel, Switzerland) Vol. 16; no. 5; p. 636
• Main Authors: Beaufrez, Jason, Guillouet, Stéphane, Seimbille, Yann, Perrio, Cécile
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 22.04.2023; MDPI
• Subjects: Acids; bioconjugation; Chemical properties; Chemical Sciences; Fluorides; Fluorine; Fluorine compounds; fluorine-18; hydrophilicity; Life Sciences; Medicinal Chemistry; Methods; PET imaging; Pharmaceutical sciences; Pharmacokinetics; Pharmacology; Potassium; pre-targeting; Radioactive tracers; Reagents; Sodium; Structure; Temperature; tetrazine; France; bioconjugation; fluorine-18; pre-targeting; PET imaging; sultone; sulfonic acid salt; tetrazine; hydrophilicity

The development of 18F-fluorotetrazines, suitable for the radiolabeling of biologics such as proteins and antibodies by IEDDA ligation, represents a major challenge, especially for pre-targeting applications. The hydrophilicity of the tetrazine has clearly become a crucial parameter for the performa...