McConathy Jonathan, Goodman Mark M
Mallinckrodt Institute of Radiology, Washington University School of Medicine, St Louis, MO, USA.
Cancer Metastasis Rev. 2008 Dec;27(4):555-73. doi: 10.1007/s10555-008-9154-7.
Amino acids are required nutrients for proliferating tumor cells, and amino acid transport is upregulated in many tumor types. Studies of radiolabeled amino acids in animals and humans demonstrate that amino acid based tracers have advantageous characteristics relative to 2-[(18)F]fluoro-2-deoxyglucose in certain tumors, particularly brain gliomas. Non-natural amino acids for tumor imaging generally have greater metabolic stability and can be labeled with longer-lived radionuclides for positron emission tomography and single photon emission computed tomography such as fluorine-18 and iodine-123. Amino acids enter cells via amino acid transport with varying selectivity based on their chemical structure. This review focuses on the rationale, biological basis, current status and future prospects of radiolabeled non-natural amino acids for tumor imaging and discusses various classes of these compounds including aromatic, alicyclic and alpha,alpha-dialkyl amino acids.
氨基酸是肿瘤细胞增殖所需的营养物质，许多肿瘤类型中氨基酸转运上调。对动物和人类放射性标记氨基酸的研究表明，在某些肿瘤，特别是脑胶质瘤中，基于氨基酸的示踪剂相对于2-[(18)F]氟-2-脱氧葡萄糖具有优势特性。用于肿瘤成像的非天然氨基酸通常具有更高的代谢稳定性，并且可以用寿命更长的放射性核素进行标记，用于正电子发射断层扫描和单光子发射计算机断层扫描，如氟-18和碘-123。氨基酸根据其化学结构通过具有不同选择性的氨基酸转运进入细胞。本综述重点关注用于肿瘤成像的放射性标记非天然氨基酸的原理、生物学基础、现状和未来前景，并讨论这些化合物的各类别，包括芳香族、脂环族和α,α-二烷基氨基酸。
