| アイテムタイプ |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2024-02-05 |
| タイトル |
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タイトル |
Preclinical Evaluation of Novel Positron Emission Tomography (PET) Probes for Imaging Leucine-Rich Repeat Kinase 2 (LRRK2) |
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言語 |
en |
| 言語 |
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言語 |
eng |
| 資源タイプ |
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資源タイプ識別子 |
http://purl.org/coar/resource_type/c_6501 |
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資源タイプ |
journal article |
| 著者 |
Zhen Chen
Jiahui chen
Mori Wakana
Yongjia Ti
Jian Rong
Yinlong Li
Erick R. Calderon Leon
Tuo Shao
Zhendong Song
Yamasaki Tomoteru
Ishii Hideki
Yiding Zhang
Tomomi Kokufuta
Kuan Hu
Xie Lin
Lee Josephson
Richard Van
Yihan Shao
Stewart Factor
Zhang Ming-Rong
Steven H. Liang
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| 抄録 |
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内容記述タイプ |
Abstract |
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内容記述 |
Parkinson’s disease (PD) is one of the most highly debilitating neurodegenerative disorders, which a!ects millions of people worldwide, and leucinerich repeat kinase 2 (LRRK2) mutations have been involved in the pathogenesis of PD. Developing a potent LRRK2 positron emission tomography (PET) tracer would allow for in vivo visualization of LRRK2 distribution and expression in PD patients. In this work, we present the facile synthesis of two potent and selective LRRK2 radioligands [11C]3 ([11C]PF-06447475) and [18F]4 ([18F]PF-06455943). Both radioligands exhibited favorable brain uptake and specific bindings in rodent autoradiography and PET imaging studies. More importantly, [18F]4 demonstrated significantly higher brain uptake in the transgenic LRRK2-G2019S mutant and lipopolysaccharide (LPS)-injected mouse models. This work may serve as a roadmap for the future design of potent
LRRK2 PET tracers. |
| 書誌情報 |
Journal of Medicinal Chemistry
発行日 2024-02
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| 出版者 |
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出版者 |
ELSEVIER |
| DOI |
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識別子タイプ |
DOI |
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関連識別子 |
10.1021/acs.jmedchem.3c01687 |
