[18F]BEAN作为代谢紊乱的潜在线粒体PET生物标志物的放射合成和体内评价。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-02-14 DOI:10.1016/j.bmcl.2025.130142

Charalambos Kaittanis , Hyunjung Kim , Tyler Teceno , Yoann Petibon , Ashley Knight , Matthew Crouthamel , Anthony P. Belanger , Zhaoming Xiong , Wanida Ruangsiriluk , Meera Modi , Rizwana Islam , Madhu Natarajan , Nikolaos Papaioannou , Christopher T. Winkelmann , Johannes Tauscher , Paul McQuade

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引用次数: 0

摘要

代谢的变化与几种常见和罕见疾病有关，如亨特综合征（MPS II）。这些变化导致线粒体功能的变化，因此使用非侵入性成像生物标志物来检测这种病理生理标志是转化医学的关键目标。在这里，我们报道了[18F]小檗碱类似物（[18F]BEAN）在野生型动物和亨特病小鼠模型中的合成和体内评价。PET/CT成像显示[18F]BEAN可以检测到亨特氏病（id KO）小鼠心脏、肝脏和大脑的线粒体功能障碍。这些数据表明[18F]BEAN可能是一种可行的翻译PET生物标志物，用于成像线粒体功能受损的各种病理。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Radiosynthesis and in vivo evaluation of [18F]BEAN as a potential mitochondria-based PET biomarker for metabolic disorders

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Radiosynthesis and in vivo evaluation of [18F]BEAN as a potential mitochondria-based PET biomarker for metabolic disorders

Changes in metabolism are associated with several prevalent and rare diseases, like Hunter syndrome (MPS II). These alterations result in changes in mitochondrial function, therefore having non-invasive imaging biomarkers to detect this pathophysiological hallmark is a key objective of translational medicine. Here we report the synthesis and in vivo evaluation of the [¹⁸F]berberine analogue ([¹⁸F]BEAN), in both wildtype animals and a mouse model of Hunter's disease. PET/CT imaging revealed that [¹⁸F]BEAN could detect mitochondrial dysfunction in the heart, liver, and brain of Hunter's disease (Ids KO) mice. These data suggest that [¹⁸F]BEAN may be a viable translational PET biomarker for the imaging of diverse pathologies that have impaired mitochondrial function.

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.