Gao Furong, Chen Jiefang, Zhou Yuancun, Cheng Letong, Hu Ming, Wang Xiaohui
Institute of Chemical Biology and Functional Molecules, State Key Laboratory of Materials-Oriented Chemical Engineering, School of Chemistry and Molecular Engineering, Nanjing Tech University Nanjing 211816 P. R. China
RSC Med Chem. 2023 Sep 14;14(11):2231-2245. doi: 10.1039/d3md00330b. eCollection 2023 Nov 15.
Alzheimer's disease (AD) is the most common form of neurodegenerative dementia. As a multifactorial disease, AD involves several etiopathogenic mechanisms, in which multiple pathological factors are interconnected with each other. This complicated and unclear pathogenesis makes AD lack effective diagnosis and treatment. Theranostics, exerting the synergistic effect of diagnostic and therapeutic functions, would provide a promising strategy for exploring AD pathogenesis and developing drugs for combating AD. With the efforts in small drug-like molecules for both diagnosis and treatment of AD, small-molecule-based theranostic agents have attracted significant attention owing to their facile synthesis, high biocompatibility and reproducibility, and easy clearance from the body through the excretion systems. In this review, the small-molecule-based theranostic agents reported in the literature for anti-AD are classified into four groups according to their diagnostic modalities. Their design rationales, chemical structures, and working mechanisms for theranostics are summarized. Finally, the opportunities for small-molecule-based theranostic agents in AD are also proposed.
阿尔茨海默病（AD）是神经退行性痴呆最常见的形式。作为一种多因素疾病，AD涉及多种致病机制，其中多种病理因素相互关联。这种复杂且不明的发病机制使得AD缺乏有效的诊断和治疗方法。诊疗一体化通过发挥诊断和治疗功能的协同效应，将为探索AD发病机制和开发抗AD药物提供一种有前景的策略。随着在用于AD诊断和治疗的类药物小分子方面的努力，基于小分子的诊疗试剂因其合成简便、生物相容性高、可重复性好以及易于通过排泄系统从体内清除而备受关注。在本综述中，文献报道的用于抗AD的基于小分子的诊疗试剂根据其诊断方式分为四类。总结了它们的设计原理、化学结构和诊疗工作机制。最后，还提出了基于小分子的诊疗试剂在AD领域的机遇。
