Department of Medical Sciences, University of Ferrara, 44121 Ferrara, Italy.
Int J Mol Sci. 2023 May 30;24(11):9465. doi: 10.3390/ijms24119465.
The discovery of the P2X7 receptor (P2X7R, originally named P2Z) in immune cells, its cloning, and the identification of its role in a multiplicity of immune-mediated diseases raised great hopes for the development of novel and more potent anti-inflammatory medicaments. Unfortunately, such hopes were partially deluded by the unsatisfactory results of most early clinical trials. This failure substantially reduced the interest of the pharmaceutical and biotech industries in the clinical development of P2X7R-targeted therapies. However, recent findings ushered in a second life for the P2X7R in diagnostic medicine. New P2X7R radioligands proved to be very reliable tools for the diagnosis of neuroinflammation in preclinical and clinical studies, and detection and measurement of free P2X7 receptor (or P2X7 subunit) in human blood suggested its potential use as a circulating marker of inflammation. Here we provide a brief review of these novel developments.
P2X7 受体（最初称为 P2Z）在免疫细胞中的发现、克隆以及其在多种免疫介导的疾病中的作用的鉴定，为开发新型、更有效的抗炎药物带来了巨大的希望。不幸的是，由于大多数早期临床试验的结果并不理想，这种希望部分落空。这一失败大大降低了制药和生物技术行业对 P2X7R 靶向治疗临床开发的兴趣。然而，最近的发现为 P2X7R 在诊断医学中的应用带来了新的契机。新的 P2X7R 放射性配体在临床前和临床研究中被证明是诊断神经炎症的非常可靠的工具，并且在人血液中检测和测量游离 P2X7 受体（或 P2X7 亚基）表明其可能作为炎症的循环标志物。在这里，我们简要回顾了这些新的发展。
Zotero 插件