Skip to main content
 
Notice: Users may be experiencing issues with displaying some pages on stanfordhealthcare.org. We are working closely with our technical teams to resolve the issue as quickly as possible. Thank you for your patience.
 

See our updated masking policy »

Stanford Health Care

Discovery of 1H-Pyrazole Biaryl Sulfonamides as Novel G2019S-LRRK2 Kinase Inhibitors. ACS medicinal chemistry letters Lesniak, R. K., Nichols, R. J., Schonemann, M., Zhao, J., Gajera, C. R., Lam, G., Nguyen, K. C., Langston, J. W., Smith, M., Montine, T. J. 2022; 13 (6): 981-988

Abstract

G2019S (GS) is the most prevalent mutation in the leucine rich repeat protein kinase 2 gene (LRRK2), a genetic predisposition that is common for Parkinson's disease, as well as for some forms of cancer, and is a shared risk allele for Crohn's disease. GS-LRRK2 has a hyperactive kinase, and although numerous drug discovery programs have targeted LRRK2 kinase, few have reached clinical development. We report the discovery and preliminary development of an entirely novel structural class of potent and selective GS-LRRK2 kinase inhibitors: biaryl-1H-pyrazoles.

View details for DOI 10.1021/acsmedchemlett.2c00116

View details for PubMedID 35707141