治疗帕金森病的富亮氨酸重复激酶 2 (LRRK2) 抑制剂:迄今为止的专利文献综述。

IF 5.4 2区 医学 Q1 CHEMISTRY, MEDICINAL Expert Opinion on Therapeutic Patents Pub Date : 2024-09-01 Epub Date: 2024-07-19 DOI:10.1080/13543776.2024.2378076
Margaux Morez, Antonio Jesús Lara Ordóñez, Patricia Melnyk, Maxime Liberelle, Nicolas Lebègue, Jean-Marc Taymans
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引用次数: 0

摘要

简介:在富亮氨酸重复激酶 2 (LRRK2) 被发现是帕金森病 (PD) 的遗传决定因素近二十年后,LRRK2 已成为帕金森病的优先治疗靶点,抑制其活性被认为是有益的:LRRK2靶向药物,特别是激酶抑制剂和减少LRRK2表达的药物在模型系统中显示出前景,并已进入治疗帕金森病的I期和II期临床试验阶段。基于促进特定的 "健康 "LRRK2四元结构、异构体复合物和构象,正在出现其他几种LRRK2靶向策略:可以预计,LRRK2靶向策略可能会在未来五年内进入治疗帕金森病的III期临床试验阶段,从而让该领域发现LRRK2靶向策略的真正临床价值。
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Leucine-rich repeat kinase 2 (LRRK2) inhibitors for Parkinson's disease: a patent review of the literature to date.

Introduction: Nearly two decades after leucine rich repeat kinase 2 (LRRK2) was discovered as a genetic determinant of Parkinson's disease (PD), LRRK2 has emerged a priority therapeutic target in PD and inhibition of its activity is hypothesized to be beneficial.

Areas covered: LRRK2 targeting agents, in particular kinase inhibitors and agents reducing LRRK2 expression show promise in model systems and have progressed to phase I and phase II clinical testing for PD. Several additional targeting strategies for LRRK2 are emerging, based on promoting specific 'healthy' LRRK2 quaternary structures, heteromeric complexes and conformations.

Expert opinion: It can be expected that LRRK2 targeting strategies may proceed to phase III clinical testing for PD in the next five years, allowing the field to discover the real clinical value of LRRK2 targeting strategies.

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来源期刊
CiteScore
12.10
自引率
1.50%
发文量
50
审稿时长
6-12 weeks
期刊介绍: Expert Opinion on Therapeutic Patents (ISSN 1354-3776 [print], 1744-7674 [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on recent pharmaceutical patent claims, providing expert opinion the scope for future development, in the context of the scientific literature. The Editors welcome: Reviews covering recent patent claims on compounds or applications with therapeutic potential, including biotherapeutics and small-molecule agents with specific molecular targets; and patenting trends in a particular therapeutic area Patent Evaluations examining the aims and chemical and biological claims of individual patents Perspectives on issues relating to intellectual property The audience consists of scientists, managers and decision-makers in the pharmaceutical industry and others closely involved in R&D Sample our Bioscience journals, sign in here to start your access, Latest two full volumes FREE to you for 14 days.
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