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

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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Abstract

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.