GNE-0877

Описание

Leucine-rich repeat kinase 2 (LRRK2) is an enzyme that interacts with parkin, a ligase that is part of the ubiquitin-proteasome system that mediates the targeting of proteins for degradation. Loss of function of the parkin protein leads to dopaminergic cell death. The development of Parkinson''s disease has been strongly associated with mutations in the LRRK2 gene that lead to increased kinase activity. GNE 0877 is a selective, brain-penetrable LRRK2 inhibitor (K_i = 0.7 nM). It inhibits LRRK2 Ser¹²⁹² autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation with an IC₅₀ value of 3 nM in vivo.

Использование

GNE-0877 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor.