Department of Chemistry, Babasaheb Bhimrao Ambedkar University, (A Central University), Lucknow, Uttar Pradesh 226025, India.
Department of Chemistry, Babasaheb Bhimrao Ambedkar University, A Central University, Lucknow, Uttar Pradesh 226025, India.
Mol Pharm. 2021 Apr 5;18(4):1507-1529. doi: 10.1021/acs.molpharmaceut.1c00002. Epub 2021 Mar 1.
Positron emission tomography (PET) imaging of the translocator 18 kDa protein (TSPO) with radioligands has become an effective means of research in peripheral inflammatory conditions that occur in many diseases and cancers. The peripheral sterile inflammatory diseases (PSIDs) are associated with a diverse group of disorders that comprises numerous enduring insults including the cardiovascular, respiratory, gastrointestinal, or musculoskeletal system. TSPO has recently been introduced as a potential biomarker for peripheral sterile inflammatory diseases (PSIDs). The major critical issue related to PSIDs is its timely characterization and localization of inflammatory for proper therapy of patients. As an alternative to metabolic imaging, protein imaging expressed on immune cells after activation is of great importance. The five transmembrane domain translocator protein-18 kDa (TSPO) is upregulated on the mitochondrial cell surface of macrophages during inflammation, serving as a potential ligand for PET tracers. Additionally, the overexpressed TSPO protein has been positively correlated with various tumor malignancies. In view of the association of escalated TSPO expression in both disease conditions, it is an immensely important biomarker for PET imaging in oncology and PSIDs. In this review, we summarize the most outstanding advances on TSPO-targeted PSIDs and cancer in the development of TSPO ligands as a potential diagnostic tool, specifically discussing the last five years.
正电子发射断层扫描（PET）成像技术通过放射性配体对转位蛋白 18 kDa（TSPO）的研究已成为研究许多疾病和癌症中发生的外周炎症状态的有效手段。外周无菌性炎症性疾病（PSIDs）与多种疾病相关，包括心血管、呼吸、胃肠道或肌肉骨骼系统等多种持续的损伤。TSPO 最近被引入作为外周无菌性炎症性疾病（PSIDs）的潜在生物标志物。与 PSIDs 相关的主要关键问题是及时对其进行炎症的特征化和定位，以便为患者提供适当的治疗。作为代谢成像的替代方法，免疫细胞激活后表达的蛋白质成像具有重要意义。跨膜域 5 转位蛋白-18 kDa（TSPO）在炎症期间在巨噬细胞的线粒体细胞表面上调，作为 PET 示踪剂的潜在配体。此外，过表达的 TSPO 蛋白与各种肿瘤恶性肿瘤呈正相关。鉴于在这两种疾病状况下 TSPO 表达的增加与疾病的相关性，TSPO 是 PSIDs 和肿瘤 PET 成像的一个非常重要的生物标志物。在这篇综述中，我们总结了 TSPO 靶向 PSIDs 和癌症方面的最新进展，将 TSPO 配体作为一种潜在的诊断工具，特别讨论了过去五年的进展。
