Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy.
Curr Top Med Chem. 2012;12(4):352-9. doi: 10.2174/156802612799078667.
The Translocator Protein (18 kDa) (TSPO), previously known as the peripheral benzodiazepine receptor, is widely expressed in glial cells and in peripheral tissues and is involved in a variety of biological processes: steroidogenesis, cell growth and differentiation, apoptosis induction, etc. TSPO basal expression is up-regulated in a number of human pathologies, including a variety of tumors and neuropathologies, such as gliomas and neurodegenerative disorders (Huntington's and Alzheimer's diseases), as well as in various forms of brain injury and inflammation. Furthermore, changes in TSPO receptor levels have been found in anxiety and mood disorders. Nowadays, considerable efforts have been focused on the identification of new TSPO ligands characterized by high-affinity and selectivity. In this review, we report and analyze the main experimental data and the computational procedures and validation methods used for the construction of the TSPO receptor and ligand-based models, describing in detail the most successful results and the new trends.
转位蛋白（18kDa）（TSPO）以前称为外周苯二氮䓬受体，广泛表达于神经胶质细胞和外周组织中，并参与多种生物学过程：类固醇生成、细胞生长和分化、细胞凋亡诱导等。在许多人类疾病中，包括各种肿瘤和神经病理学，如神经胶质瘤和神经退行性疾病（亨廷顿氏病和阿尔茨海默病），以及各种形式的脑损伤和炎症中，TSPO 基础表达上调。此外，在焦虑和情绪障碍中也发现 TSPO 受体水平发生变化。如今，人们已经投入大量精力来鉴定具有高亲和力和选择性的新型 TSPO 配体。在这篇综述中，我们报告和分析了构建 TSPO 受体和配体模型的主要实验数据以及计算程序和验证方法，详细描述了最成功的结果和新趋势。
