Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (BHU), Varanasi, U.P.-221005, India.
Molecular Science Laboratory, National Institute of Immunology, New Delhi-110067, India.
J Med Chem. 2022 Jul 14;65(13):8550-8595. doi: 10.1021/acs.jmedchem.1c01619. Epub 2022 Jun 27.
A person suspected of having Alzheimer's disease (AD) is clinically diagnosed for the presence of principal biomarkers, especially misfolded amyloid-beta (Aβ) and tau proteins in the brain regions. Existing radiotracer diagnostic tools, such as PET imaging, are expensive and have limited availability for primary patient screening and pre-clinical animal studies. To change the status quo, small-molecular near-infrared (NIR) probes have been rapidly developed, which may serve as an inexpensive, handy imaging tool to comprehend the dynamics of pathogenic progression in AD and assess therapeutic efficacy . This Perspective summarizes the biochemistry of Aβ and tau proteins and then focuses on structurally diverse NIR probes with coverages of their spectroscopic properties, binding affinity toward Aβ and tau species, and theranostic effectiveness. With the summarized information and perspective discussions, we hope that this paper may serve as a guiding tool for designing novel imaging fluoroprobes with theranostic capabilities in the future.
疑似阿尔茨海默病（AD）的患者在临床上通过主要生物标志物进行诊断，尤其是大脑区域中错误折叠的淀粉样蛋白-β（Aβ）和 tau 蛋白。现有的放射性示踪剂诊断工具，如 PET 成像，昂贵且在对原发性患者进行筛查和临床前动物研究方面的可用性有限。为了改变这种现状，小分子近红外（NIR）探针得到了快速发展，它们可能成为一种廉价、便捷的成像工具，用于了解 AD 发病进展的动态，并评估治疗效果。本文综述了 Aβ和 tau 蛋白的生物化学特性，然后重点介绍了结构多样的 NIR 探针，涵盖了它们的光谱特性、对 Aβ和 tau 物种的结合亲和力以及治疗效果。通过总结的信息和观点讨论，我们希望本文可以为设计具有治疗潜力的新型成像荧光探针提供指导。
