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一步法合成 F 标记的硼代蛋氨酸类似物:C 蛋氨酸的替代品?

One-step synthesis of an F-labeled boron-derived methionine analog: a substitute for C-methionine?

机构信息

Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.

Hubei Key Laboratory of Molecular Imaging, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.

出版信息

Eur J Nucl Med Mol Imaging. 2018 Apr;45(4):582-584. doi: 10.1007/s00259-017-3927-6. Epub 2018 Jan 18.

Abstract

Amino acid-based tracers have been extensively investigated for positron emission tomography (PET) imaging of brain tumors, and C-methionine (C-MET) is one of the most extensively investigated. However, widespread clinical use of C-MET is challenging due to the short half-life of C and low radiolabeling yield. In this issue of the European Journal of Nuclear Medicine and Molecular Imaging, Yang and colleagues report an F-labeled boron-derived methionine analog, F-B-MET, as a potential substitute for C-MET in PET imaging of glioma. The push-button synthesis, highly efficient radiolabeling, and good imaging performance in glioma models make this tracer a promising candidate for future clinical translation.

摘要

氨基酸类示踪剂已广泛应用于脑肿瘤的正电子发射断层扫描(PET)成像研究,其中 C-蛋氨酸(C-MET)是研究最多的示踪剂之一。然而,由于 C 的半衰期短和放射性标记产率低,C-MET 的广泛临床应用具有挑战性。在本期《欧洲核医学与分子影像杂志》中,Yang 及其同事报道了一种 F 标记的硼衍生蛋氨酸类似物 F-B-MET,可作为 C-MET 在脑胶质瘤 PET 成像中的潜在替代物。该示踪剂具有一键式合成、高效放射性标记和良好的脑胶质瘤模型成像性能,有望成为未来临床转化的候选药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d71e/5831531/7ae63181ec52/nihms931264f1.jpg

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