Design and Synthesis of Pyrrolo[2,3-<i>d</i>]pyrimidine-Derived Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Checkpoint Kinase 1 (CHK1)-Derived Crystallographic Surrogate
D.S. Williamson, Garrick P. Smith, Gitte Kobberøe Mikkelsen, Thomas Jensen, P. Acheson-Dossang, Lassina Badolo, Simon T. Bedford, Victoria Chell, I‐Jen Chen, P. Dokurno, Morten Hentzer, Samantha Newland, Stuart Ray, T. Shaw, A.E. Surgenor, Lindsey Terry, Yikang Wang, Kenneth Vielsted Christensen
Abstract
demonstrated high potency and exquisite selectivity for LRRK2 and utility as chemical probes for the study of LRRK2 inhibition.
Topics & Concepts
ChemistryLRRK2KinaseProtein kinase domainStereochemistryLeucine-rich repeatPotencyIn vivoMutantBiochemistryIn vitroMutationBiologyGeneBiotechnologyParkinson's Disease Mechanisms and TreatmentsMicrobial Natural Products and BiosynthesisFungal and yeast genetics research