Leucine-rich repeat kinase 2 (LRRK2) inhibitors for Parkinson's disease: a patent review of the literature to date

被引：6

作者：

Morez, Margaux ^{[1
]}

Ordonez, Antonio Jesus Lara ^{[1
]}

Melnyk, Patricia ^{[1
]}

Liberelle, Maxime ^{[1
]}

Lebegue, Nicolas ^{[1
]}

Taymans, Jean-Marc ^{[1
]}

机构：

[1] Univ Lille, U1172, LilNCog, Lille Neurosci & Cognit,INSERM,CHU Lille, Lille, France

来源：

EXPERT OPINION ON THERAPEUTIC PATENTS | 2024年 / 34卷 / 09期

关键词：

LRRK2; kinase; allosteric; GTPase; Parkinson's disease; conformation; ALPHA-SYNUCLEIN; 14-3-3; BINDING; MUTATIONS; G2019S; PHOSPHORYLATION; IDENTIFICATION; DOMAIN; LUNG; ROC;

D O I：

10.1080/13543776.2024.2378076

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

IntroductionNearly 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 coveredLRRK2 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 opinionIt 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.

引用

页码：773 / 788

页数：16

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