Christophe Peixoto, Agnes Joncour, Taouès Temal-Laib, Amynata Tirera, Aurélie Dos Santos, Hélène Jary, Denis Bucher, Wendy Laenen, Anna Pereira Fernandes, Stephanie Lavazais, Carole Delachaume, Didier Merciris, Corinne Saccomani, Michael Drennan, Miriam López-Ramos, Emanuelle Wakselman, Sonia Dupont, Monica Borgonovi, Carlos Roca Magadan, Alain Monjardet, Reginald Brys, Steve De Vos, Martin Andrews, Juan-Miguel Jimenez, David Amantini, Nicolas Desroy
The salt-inducible kinases (SIKs) SIK1, SIK2, and SIK3 belong to the adenosine monophosphate-activated protein kinase (AMPK) family of serine/threonine kinases. SIK inhibition represents a new therapeutic approach modulating pro-inflammatory and immunoregulatory pathways that holds potential for the treatment of inflammatory diseases. Here, we describe the identification of GLPG3970 ( 32 ), a first-in-class dual SIK2/SIK3 inhibitor with selectivity against SIK1 (IC50 of 282.8 nM on SIK1, 7.8 nM on SIK2 and 3...
March 29, 2024: Journal of Medicinal Chemistry