Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA.
Curr Top Med Chem. 2013;13(8):871-91. doi: 10.2174/1568026611313080002.
(18)F-labeled amino acids are an important class of imaging agents for positron emission tomography (PET) that target the increased rates of amino acid transport by many tumor cells. This class of tracers is structurally diverse, and the biological and imaging properties of a given (18)F-labeled amino acid depends largely upon its mechanism of transport. The system L amino acid transport system has been a major focus of tracer development in this field, but more recently (18)F-labeled amino acids have been developed for other transporters including system A, glutamine, glutamate and cationic amino acid transport systems. Radiolabeled amino acids are best established for brain tumor imaging, but there are emerging applications in other types of cancer such as neuroendocrine tumors and prostate cancer. This review provides an overview of (18)F-labeled amino acids for oncologic imaging in terms of design considerations, radiosynthetic methods, and key clinical applications.
(18)F 标记的氨基酸是正电子发射断层扫描(PET)成像剂的一个重要类别,针对许多肿瘤细胞氨基酸转运率的增加。这类示踪剂具有结构多样性,特定的(18)F 标记氨基酸的生物学和成像特性在很大程度上取决于其转运机制。系统 L 氨基酸转运系统一直是该领域示踪剂开发的主要焦点,但最近(18)F 标记的氨基酸已针对其他转运体(包括系统 A、谷氨酰胺、谷氨酸和阳离子氨基酸转运系统)进行了开发。放射性标记的氨基酸在脑肿瘤成像方面的应用最为成熟,但在其他类型的癌症(如神经内分泌肿瘤和前列腺癌)中也有新的应用。本综述从设计考虑、放射合成方法和关键临床应用等方面,概述了用于肿瘤成像的(18)F 标记氨基酸。