Chemical Biology of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors

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• 作者：Anthony A. Estrada ; Zachary K. Sweeney
• 刊名：Journal of Medicinal Chemistry
• 出版年：2015
• 出版时间：September 10, 2015
• 年：2015
• 卷：58
• 期：17
• 页码：6733-6746
• 全文大小：536K
• ISSN：1520-4804

文摘

There is an urgent need for the development of Parkinson鈥檚 disease (PD) treatments that can slow disease progression. The leucine-rich repeat kinase 2 (LRRK2) protein has been genetically and functionally linked to PD, and modulation of LRRK2 enzymatic activity has been proposed as a novel therapeutic strategy. In this review, we describe the bioactivity of selected small molecules that have been used to inhibit LRRK2 kinase activity in vitro or in vivo. These compounds are important tools for understanding the cellular biology of LRRK2 and for evaluating the potential of LRRK2 inhibitors as disease-modifying PD therapies.