Haskali Mohammad B, Roselt Peter D, Hicks Rodney J, Hutton Craig A
School of Chemistry, The University of Melbourne, Melbourne, Victoria, Australia.
Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, Victoria, Australia.
J Labelled Comp Radiopharm. 2018 Feb;61(2):61-67. doi: 10.1002/jlcr.3580. Epub 2017 Dec 29.
Radiolabelled peptides are vital tools used in positron emission tomography imaging for the diagnosis of disease, drug discovery, and biomedical research. Peptides are typically labeled through conjugation to a radiolabelled prosthetic group, which usually necessitates complex, multi-step procedures, especially for fluorine-18 labeled peptides. Herein, we describe the automated synthesis and formulation of 2-[ F]fluoropropionate labeled RGD-peptides through use of the iPHASE Flexlab as an effective dual-stage radiochemical synthesis module. The fully automated preparation of the monomeric RGD-peptides, [ F]FP-GalactoRGD and [ F]FP-c(RGDy(SO )K), was accomplished in under 90 minutes with n.d.c. radiochemical yields ca. 7% from fluoride. Similarly, the automated preparation of the dimeric RGD-peptides, [ F]F-PRGD and [ F]FP-E(RGDy(SO )K) , was accomplished in under 105 minutes with n.d.c. yields ca. 4% from fluoride.
放射性标记肽是正电子发射断层扫描成像中用于疾病诊断、药物研发和生物医学研究的重要工具。肽通常通过与放射性标记的辅基结合进行标记，这通常需要复杂的多步程序，尤其是对于氟-18标记的肽。在此，我们描述了通过使用iPHASE Flexlab作为有效的双阶段放射化学合成模块，自动合成和配制2-[F]氟丙酸酯标记的RGD肽。单体RGD肽[F]FP-GalactoRGD和[F]FP-c(RGDy(SO)K)的全自动制备在90分钟内完成，非衰变校正放射化学产率约为7%（基于氟化物）。同样，二聚体RGD肽[F]F-PRGD和[F]FP-E(RGDy(SO)K)的自动制备在105分钟内完成，非衰变校正产率约为4%（基于氟化物）。
