Peptides Radiofluorination: Main Methods and Highlights
Peptides Radiofluorination: Main Methods and Highlights作者机构：Radiopharmaceutical Research and Production Unit Nuclear Technology Development Center Belo Horizonte Brazil Anatomy and Imaging Department Faculty of Medicine Federal University of Minas Gerais Belo Horizonte Brazil
出 版 物：《International Journal of Organic Chemistry》 (有机化学国际期刊（英文）)
年 卷 期：2022年第12卷第4期
页 面：161-172页
学科分类：081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学]
主 题：Radiofluorination Radiolabeling Peptides Prosthetic Groups Fluorine-18
摘 要：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.
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