期刊
PHARMACEUTICS
卷 14, 期 11, 页码 -出版社
MDPI
DOI: 10.3390/pharmaceutics14112545
关键词
translocator protein; TSPO ligands; PET; neuroinflammation; molecular imaging
资金
- National Research Foundation of Korea (NRF) - Korea government (MSIT)
- [NRF-2021R1A2C1011204]
TSPO plays important roles in cellular functions and its abnormal expression is associated with pathological disorders, making it a biomarker for related diseases. PET, as a non-invasive imaging technique, can detect diseases related to TSPO expression. Recent studies have focused on the development of F-18-labeled TSPO as PET tracers.
Translocator protein 18 kDa (TSPO) is a transmembrane protein in the mitochondrial membrane, which has been identified as a peripheral benzodiazepine receptor. TSPO is generally present at high concentrations in steroid-producing cells and plays an important role in steroid synthesis, apoptosis, and cell proliferation. In the central nervous system, TSPO expression is relatively modest under normal physiological circumstances. However, some pathological disorders can lead to changes in TSPO expression. Overexpression of TSPO is associated with several diseases, such as neurodegenerative diseases, neuroinflammation, brain injury, and cancers. TSPO has therefore become an effective biomarker of related diseases. Positron emission tomography (PET), a non-invasive molecular imaging technique used for the clinical diagnosis of numerous diseases, can detect diseases related to TSPO expression. Several radiolabeled TSPO ligands have been developed for PET. In this review, we describe recent advances in the development of TSPO ligands, and F-18-radiolabeled TSPO in particular, as PET tracers. This review covers pharmacokinetic studies, preclinical and clinical trials of F-18-labeled TSPO PET ligands, and the synthesis of TSPO ligands.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据