显像α-突触核蛋白病的PET示踪剂开发

IF 6.9 3区 医学 Q1 CHEMISTRY, MEDICINAL
Mohammad Maqusood Alam, Sun Hak Lee, Sobia Wasim, Sang-Yoon Lee
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引用次数: 0

摘要

α-突触核蛋白异常聚集是α-突触核蛋白病(如帕金森病(PD)、多系统萎缩(MSA)等神经系统疾病)的关键神经病理学标志,与发病机制密切相关。α-突触核蛋白病的主要特征是选择性靶向性神经变性和Lewy病变的积累。具体来说,α-突触核蛋白正电子发射断层扫描(PET)示踪剂靶向蛋白的纤维形态,从而增强了对各种α-突触核蛋白病的早期诊断和治疗效果评估。因此,使用靶向放射性标记探针在体内检测α-突触核蛋白聚集体将有助于药物开发、早期诊断和持续的疾病监测。因此,目前尚无适合临床应用的α-突触核蛋白生物标志物的报道。PET是一种有价值的非侵入性技术,用于成像药物在活体动物和人类组织中的分布和受体在靶部位的占用。PET生物标记物的进展显著增强了我们对PD机制的理解。本文综述了近年来α-突触核蛋白选择性PET示踪剂的研究进展,并对其发展前景进行了展望。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
PET tracer development for imaging α-synucleinopathies

Abnormal α-synuclein aggregation is a key neuropathological hallmark of α-synucleinopathies, such as Parkinson’s disease (PD), multiple system atrophy (MSA), and several other neurological disorders, and closely contributes to pathogenesis. The primary characteristics of α-synucleinopathies are selective targeted neurodegeneration and the accumulation of Lewy pathologies. Specifically, α-synuclein positron emission tomography (PET) radiotracers target the fibrillar forms of the protein, thus enhancing early diagnosis and the evaluation of treatment effectiveness for various α-synucleinopathies. Therefore, in vivo detection of α-synuclein aggregates using targeted radiolabeled probes would aid in drug development, early diagnosis, and ongoing disease monitoring. As such, no promising α-synuclein biomarkers suitable for clinical applications have been reported. PET is a valuable non-invasive technique for imaging drug distribution in tissues and receptor occupancy at target sites in living animals and humans. Advances in PET biomarkers have significantly enhanced our understanding of the mechanisms underlying PD. This review summarizes recent ongoing efforts in the development of selective PET tracers for α-synuclein and discusses future perspectives.

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来源期刊
CiteScore
13.40
自引率
9.00%
发文量
48
审稿时长
3.3 months
期刊介绍: Archives of Pharmacal Research is the official journal of the Pharmaceutical Society of Korea and has been published since 1976. Archives of Pharmacal Research is an interdisciplinary journal devoted to the publication of original scientific research papers and reviews in the fields of drug discovery, drug development, and drug actions with a view to providing fundamental and novel information on drugs and drug candidates.
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