Juraj Velcicky, Philipp Janser, Nina Gommermann, Silke Brenneisen, Slavica Ilic, Eric Vangrevelinghe, Nikolaus Stiefl, Andreas Boettcher, Christelle Arnold, Claire Malinverni, Janet Dawson, Renata Murgasova, Sandrine Desrayaud, Karen Beltz, Alexandra Hinniger, Carien Dekker, Christopher J Farady, Angela Mackay
NLRP3 is a molecular sensor recognizing a wide range of danger signals. Its activation leads to the assembly of an inflammasome that allows for activation of caspase-1 and subsequent maturation of IL-1β and IL-18, as well as cleavage of Gasdermin-d and pyroptotic cell death. The NLRP3 inflammasome has been implicated in a plethora of diseases including gout, type 2 diabetes, atherosclerosis, Alzheimer's disease, and cancer. In this publication, we describe the discovery of a novel, tricyclic, NLRP3-binding scaffold by high-throughput screening...
January 4, 2024: Journal of Medicinal Chemistry