Pharmacological inhibition of CaMKK2 with the selective antagonist STO-609 regresses NAFLD.

ABSTRACT: Binding of calcium to its intracellular receptor calmodulin (CaM) activates a family of Ca²⁺/CaM-dependent protein kinases. CaMKK2 (Ca²⁺/CaM-dependent protein kinase kinase 2) is a central member of this kinase family as it controls the actions of a CaMK cascade involving CaMKI, CaMKIV or AMPK. CaMKK2 controls insulin signaling, metabolic homeostasis, inflammation and cancer cell growth highlighting its potential as a therapeutic target for a variety of diseases. STO-609 is a selective, small molecule inhibitor of CaMKK2. Although STO-609 has been used extensively in vitro and in cells to characterize and define new mechanistic functions of CaMKK2, only a few studies have reported the in vivo use of STO-609. We synthesized functional STO-609 and assessed its pharmacol

SUBMITTER: York B 

PROVIDER: S-EPMC5603587 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature