Article
Discovery of MK-1468: A Potent, Kinome-Selective, Brain-Penetrant Amidoisoquinoline LRRK2 Inhibitor for the Potential Treatment of Parkinson's Disease.
Journal of medicinal chemistry - 9 Nov 2023
Kattar Solomon D, Gulati Anmol, Margrey Kaila A, Keylor Mitchell H, Ardolino Michael, Yan Xin, Johnson Rebecca, Palte Rachel L, McMinn Spencer E, Nogle Lisa, Su Jing, Xiao Dong, Piesvaux Jennifer, Lee Susi, Hegde Laxminarayan G, Woodhouse Janice D, Faltus Robert, Moy Lily Y, Xiong Tina, Ciaccio Paul J, Pearson Kara, Patel Mayankbhai, Otte Karin M, Leyns Cheryl E G, Kennedy Matthew E, Bennett David Jonathan, DiMauro Erin F, Fell Matthew J, Fuller Peter H
Abstract excerpt
Genetic mutation of the leucine-rich repeat kinase 2 (LRRK2) protein has been associated with Parkinson's disease (PD), a disabling and progressive neurodegenerative disorder that is devoid of efficacious disease-modifying therapies. Herein, we describe the invention of an amidoisoquinoline (IQ)-derived LRRK2 inhibitor lead chemical series. Knowledge-, structure-, and property-based drug design in concert with...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.