诊断性放射性药物靶点的成药潜力
Druggability of Targets for Diagnostic Radiopharmaceuticals.
作者信息
Wang Xinyu, Chen Chongyang, Yan Junjie, Xu Yuping, Pan Donghui, Wang Lizhen, Yang Min
机构信息
NHC Key Laboratory of Nuclear Medicine, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, PR China.
School of Pharmacy, Nanjing Medical University, Nanjing 211166, PR China.
出版信息
ACS Pharmacol Transl Sci. 2023 Jul 12;6(8):1107-1119. doi: 10.1021/acsptsci.3c00081. eCollection 2023 Aug 11.
Targets play an indispensable and pivotal role in the development of radiopharmaceuticals. However, the initial stages of drug discovery projects are often plagued by frequent failures due to inadequate information on druggability and suboptimal target selection. In this context, we aim to present a comprehensive review of the factors that influence target druggability for diagnostic radiopharmaceuticals. Specifically, we explore the crucial determinants of target specificity, abundance, localization, and positivity rate and their respective implications. Through a detailed analysis of existing protein targets, we elucidate the significance of each factor. By carefully considering and balancing these factors during the selection of targets, more efficacious and targeted radiopharmaceuticals are expected to be designed for the diagnosis of a wide range of diseases in the future.
靶点在放射性药物的研发中起着不可或缺且至关重要的作用。然而，由于关于成药可能性的信息不足以及靶点选择欠佳，药物研发项目的初始阶段常常频繁遭遇失败。在此背景下，我们旨在全面综述影响诊断性放射性药物靶点成药可能性的因素。具体而言，我们探讨靶点特异性、丰度、定位及阳性率的关键决定因素及其各自的影响。通过对现有蛋白质靶点的详细分析，我们阐明每个因素的重要性。在靶点选择过程中仔细考虑并平衡这些因素，有望在未来设计出更有效且靶向性更强的放射性药物用于多种疾病的诊断。
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