Development of [¹⁸F]AmBF₃ Tetrazine for Radiolabeling of Peptides: Preclinical Evaluation and PET Imaging of [¹⁸F]AmBF₃-PEG₇-Tyr³-Octreotide in an AR42J Pancreatic Carcinoma Model.

ABSTRACT: Radiolabeled peptides have emerged as highly specific agents for targeting receptors expressed in tumors for therapeutic and diagnostic purposes. Peptides developed for positron emission tomography (PET) are typically radiolabeled using prosthetic groups or bifunctional chelators for fast "kit-like" incorporation of the radionuclide into the structure. A novel [¹⁸F]alkylammoniomethyltrifluoroborate ([¹⁸F]AmBF₃) tetrazine (Tz), [¹⁸F]AmBF₃-Tz, was developed for the [¹⁸F]fluorination of trans-cyclooctene (TCO)-modified biomolecules using Tyr³-octreotides (TOCs) as model peptides. [¹⁸F]AmBF₃-Tz (A_m = 15.4 ± 9.2 GBq/μmol, n = 14) was evaluated in healthy mice by ex vivo

SUBMITTER: Otaru S 

PROVIDER: S-EPMC9305971 | biostudies-literature | 2022 Jul

REPOSITORIES: biostudies-literature