PDF(Pubmed)
Abstract：
The translocator protein 18-kDa (TSPO) is a mitochondrial membrane protein that is previously identified as the peripheral benzodiazepine receptor (PBR). Furthermore, it plays a significant role in a diverse range of biochemical processes, including steroidogenesis, mitochondrial cholesterol transport, cell survival and death, cell proliferation, and carcinogenesis. Several investigations also reported its roles in various types of cancers, including colorectal, brain, breast, prostate, and lung cancers, as well as melanoma. According to a previous study, the expression of TSPO was upregulated in cancer cells, which corresponds to an aggressive phenotype and/or poor prognosis. Consequently, the potential for crafting diagnostic and prognostic tools with a focus on TSPO holds great potential. In this context, several radioligands designed to target this protein have been identified, and some of the candidates have advanced to clinical trials. In recent years, the use of hybrid probes with radioactive and fluorescence molecules for image-guided surgery has exhibited promising results in animal and human studies. This indicates that the approach can serve as a valuable surgical navigator during cancer surgery. The current hybrid probes are built from various molecular platforms, including small molecules, nanoparticles, and antibodies. Although several TSPO-targeted imaging probes have been developed, their development for image-guided surgery of cancers is still limited. Therefore, this review aims to highlight recent findings on the involvement of TSPO in carcinogenesis, as well as provide a new perspective on the potential application of TSPO-targeted hybrid probes for image-guided surgery.
摘要：
转运蛋白18-kDa（TSPO）是一种线粒体膜蛋白，先前被鉴定为外周苯二氮卓受体（PBR）。此外，它在各种生化过程中发挥着重要作用，包括类固醇生成，线粒体胆固醇转运，细胞生存和死亡，细胞增殖，和致癌作用。一些调查还报告了它在各种类型的癌症中的作用，包括结直肠,大脑,乳房,前列腺,肺癌，以及黑色素瘤。根据之前的一项研究,TSPO在癌细胞中的表达上调,这对应于侵袭性表型和/或不良预后。因此,以TSPO为重点制作诊断和预后工具的潜力巨大。在这种情况下，已经鉴定出几种针对这种蛋白质的放射性配体，一些候选人已经进入临床试验。近年来,将具有放射性和荧光分子的混合探针用于图像引导的手术在动物和人类研究中显示出有希望的结果。这表明该方法可以在癌症手术期间用作有价值的手术导航仪。目前的杂交探针由各种分子平台构建而成，包括小分子，纳米粒子，和抗体。尽管已经开发了几种TSPO靶向成像探针，它们在癌症图像引导手术中的发展仍然有限。因此,这篇综述旨在强调TSPO参与癌变的最新发现，以及为TSPO靶向混合探针在图像引导手术中的潜在应用提供了新的视角。
