Leucine-rich repeat kinase 2 inhibitor as Parkinson′s disease novel therapeutics:research advances
10.13220/j.cnki.jipr.2016.01.014
- VernacularTitle:富亮氨酸重复激酶2抑制剂作为新型帕金森病治疗剂的研究进展
- Author:
Xiaoyu ZHAN
;
Xuhong REN
;
Xinhua HE
- Publication Type:Journal Article
- Keywords:
Parkinson′s disease;
leucine-rich repeat kinase 2;
leucine-rich repeat kinase 2 inhibitor;
kinase binding site;
GTP binding site
- From:
Journal of International Pharmaceutical Research
2016;(1):97-103,133
- CountryChina
- Language:Chinese
-
Abstract:
Parkinson′s disease(PD)is a common disease caused by multiple factors and characterized by pathological degen?eration in the dopaminergic neural system. Based on its pathogenic factors,PD can be divided into several subtypes,so it is essential to develop therapeutic agents based on the main pathogenic factor of each subtype of PD. Recently it is confirmed that the mutation of leucine-rich repeat kinase 2(LRRK2)gene leads to increased activity of the LRRK2 notably,and then causes neurodegeneration. Thus developing LRRK2 inhibitors to modulate the kinase activity will be a novel therapy for the PD subtype which is caused by LRRK2 gene mutation. LRRK2,either a kinase or a GTPase,has two drug binding sites. Therefore,two types of LRRK2 inhibitors are being studied,one is the kinase inhibitor and the other is GTPase inhibitor. This paper summarizes the recent progress in the dis?covery and development of LRRK2 inhibitors.
