Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable, and Blood–Brain Barrier Penetrant PROTAC Degrader of Leucine-Rich Repeat Kinase 2
Xingui Liu, Alexia F. Kalogeropulou, Sofia Domingos, Nikolai Makukhin, Raja Sekhar Nirujogi, François Singh, Natalia Shpiro, Anton Saalfrank, Esther Sammler, Ian G. Ganley, Rui Moreira, Dario R. Alessi, Alessio Ciulli
Abstract
and offer an attractive starting point for future drug development.
Topics & Concepts
ChemistryPenetrant (biochemical)BioavailabilityBlood–brain barrierPharmacologyKinaseBiochemistryCentral nervous systemOrganic chemistryNeurosciencePsychologyMedicineProtein Degradation and InhibitorsUbiquitin and proteasome pathwaysPeptidase Inhibition and Analysis