Deep Chatterjee

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.

2 months ago | dx.doi.org | Sebastian Mandel |Thomas Hanke |Sebastian Mathea |Deep Chatterjee

IntroductionClick to copy section linkSection link copied!Protein kinases form a large family of proteins with largely conserved ATP binding sites. Their pivotal role in the development of diseases led to their extensive exploitation as drug targets. To date, protein kinases are one of the most successful protein families for the development of new medicines.