Tempra Giorgia, Matera Carlo
Department of Pharmaceutical Sciences, University of Milan, Milan, 20133, Italy.
Purinergic Signal. 2025 May 9. doi: 10.1007/s11302-025-10094-7.
This Journal Club article reviews a 2025 study by Qiu et al. that reports the development of a novel iodine-125 radioligand targeting the purinergic P2X7 receptor (P2X7R). The researchers created a small library of structurally modified P2X7R antagonists and identified compound 1c as a lead due to its high affinity and selectivity. Radiolabeling with iodine-125 produced [I]1c with high yield and purity. Binding studies confirmed its strong nanomolar affinity, supporting its use in radioligand screening and potential applications in imaging P2X7R in inflammatory and neurodegenerative diseases. The study demonstrates the value of radiolabeled probes in drug discovery and purinergic signaling research.
这篇期刊俱乐部文章回顾了邱等人2025年的一项研究，该研究报告了一种靶向嘌呤能P2X7受体（P2X7R）的新型碘-125放射性配体的开发。研究人员创建了一个结构修饰的P2X7R拮抗剂小型文库，并确定化合物1c因其高亲和力和选择性而作为先导化合物。用碘-125进行放射性标记产生了高产率和高纯度的[I]1c。结合研究证实了其强纳摩尔亲和力，支持其在放射性配体筛选中的应用以及在炎症和神经退行性疾病中对P2X7R成像的潜在应用。该研究证明了放射性标记探针在药物发现和嘌呤能信号研究中的价值。
