Chin, J. (2013) Methods for Carbon-11 and Fluorine-18 Labeling of Peptides as PET Radiopharmaceuticals: Direct Labeling with [11C]Methyl Triflate on Cysteine Residues and [18F]Fluoride on the Cationic Silicon-Based Fluoride Acceptor (SIFA) Moiety. Department of Chemistry, McGill University, Montreal.

has been cited by the following article:

• TITLE: Peptides Radiofluorination: Main Methods and Highlights

  AUTHORS: Ana Carolina A. Bispo, Fernanda A. F. Almeida, Juliana B. Silva, Marcelo Mamede

  KEYWORDS: Radiofluorination, Radiolabeling, Peptides, Prosthetic Groups, Fluorine-18

  JOURNAL NAME: International Journal of Organic Chemistry, Vol.12 No.4, December 2, 2022

  ABSTRACT: Peptides have an important role in organism and its high quantity present in tumors leading to development of radiolabeled peptides for tumor-specific imaging. Once the traditional methodologies used for radiofluorination do not work with peptides, due to their harsh conditions, other radiolabeling strategies had to be developed to supply the need. Direct radiofluorination is either an inefficient method, and the use of bidirectional groups, or prosthetic groups, is needed to enable the binding between the radionuclide fluorine-18 and a peptide functionalized. New peptides radiolabeling strategies have been developed sourcing increase the synthesis yield, its chemoselectivity, and the binding stability, and reduce the total process time and the number of steps required. The progress of radiofluorination methodologies led to development of the amidation, acylation, imidation, and alkylation techniques, the use of thiol groups, photochemical conjugation, chemoselective reactions, and “click chemistry”, in addition to use of FDG molecule and heteroatoms as linkers. This paper presents the main strategies used for peptides radiofluorination, presenting their positive and negative points, and the prosthetic groups most used in each method.