64Cu-labeled phosphonium cations as PET radiotracers for tumor imaging.
64Cu-labeled phosphonium cations as PET radiotracers for tumor imaging.
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DOI：
10.1021/bc200106p
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发表时间：
2011-08-17
影响因子：
4.7
通讯作者：
Liu, Shuang
中科院分区：
文献类型：
--
作者：
Zhou, Yang;Liu, Shuang
线粒体跨膜电位（ΔΨm）的改变是癌症的一个重要特征。增强的线粒体负电位在肿瘤细胞表型中普遍存在的观察结果为开发线粒体靶向治疗药物和分子成像探针提供了概念基础。由于血浆和线粒体电位为负，许多离域有机阳离子（例如罗丹明-123 和 3H-四苯基鏻）通过电泳驱动穿过这些膜，并能够定位在肿瘤细胞的通电线粒体中。阳离子放射性示踪剂，例如99mTc-Sestamibi和99mTc-Tetrofosmin，已在临床上用于通过单光子发射计算机断层扫描（SPECT）和无创监测不同来源肿瘤的多药耐药性（MDR）转运功能来诊断癌症。然而，由于肿瘤定位不足（放射性示踪剂肿瘤摄取低）以及胸部和腹部区域放射性积累高（肿瘤选择性低），它们的诊断和预后价值通常受到限制。相比之下，64Cu标记的鏻阳离子代表了一类新型PET（正电子发射断层扫描）放射性示踪剂，具有良好的肿瘤摄取和高肿瘤选择性。这篇综述文章将重点介绍我们最近评估 64Cu 标记的鏻阳离子作为潜在 PET 放射性示踪剂的经验。主要目的是说明放射性金属螯合物对64Cu放射性示踪剂的物理、化学和生物性质的影响。它还将讨论与它们的肿瘤选择性和可能的肿瘤定位机制相关的一些重要问题。
Alteration in mitochondrial transmembrane potential (ΔΨm) is an important characteristic of cancer. The observation that the enhanced negative mitochondrial potential is prevalent in tumor cell phenotype provides a conceptual basis for development of mitochondrion-targeting therapeutic drugs and molecular imaging probes. Since plasma and mitochondrial potentials are negative, many delocalized organic cations, such as rhodamine-123 and 3H-tetraphenylphosphonium, are electrophoretically driven through these membranes, and able to localize in the energized mitochondria of tumor cells. Cationic radiotracers, such as 99mTc-Sestamibi and 99mTc-Tetrofosmin, have been clinically used for diagnosis of cancer by single photon emission computed tomography (SPECT) and noninvasive monitoring of the multidrug resistance (MDR) transport function in tumors of different origin. However, their diagnostic and prognostic values are often limited due to their insufficient tumor localization (low radiotracer tumor uptake) and high radioactivity accumulation in the chest and abdominal regions (low tumor selectivity). In contrast, the 64Cu-labeled phosphonium cations represent a new class of PET (positron emission tomography) radiotracers with good tumor uptake and high tumor selectivity. This review article will focus on our recent experiences in evaluation of 64Cu-labeled phosphonium cations as potential PET radiotracers. The main objective is to illustrate the impact of radiometal chelate on physical, chemical and biological properties of 64Cu radiotracers. It will also discuss some important issues related to their tumor selectivity and possible tumor localization mechanism.
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影响因子：
3.1
作者：
Chen, XY;Liu, S;Conti, PS
通讯作者：
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