Nicolai D Raig

3 weeks ago | science.org | Antoine Régimbeau |Martin Kihoulou |Yubei Xiang |Nicolai D Raig |Katherine J. Surridge |Marta Sanz-Murillo | +11 more

AbstractIncreased kinase activity of leucine-rich repeat kinase 2 (LRRK2) is associated with Parkinson’s disease (PD). Numerous LRRK2-selective type I kinase inhibitors have been developed, and some have entered clinical trials. Here, to our knowledge, we present the first type II kinase inhibitors that target LRRK2. Targeting the inactive conformation of LRRK2 is functionally distinct from targeting the active-like conformation using type I inhibitors.