SIK3 activator

SIK3 activators are a class of therapeutic agents designed to restore or enhance the activity of Salt-Inducible Kinase 3 (SIK3). This strategy is primarily being investigated for the treatment of cancers harboring mutations in the STK11 (also known as LKB1) tumor suppressor gene. STK11 is a master kinase that regulates downstream SIK kinases; its loss leads to reduced SIK activity, which drives tumor progression. Research by Tango Therapeutics, utilizing gain-of-function cDNA screens, identified SIK3 as a critical effector whose activation can mimic the tumor-suppressive transcriptional effects of STK11 re-expression. Preclinical studies have demonstrated that genetic or pharmacological activation of SIK3 significantly inhibits tumor growth in STK11-mutant models, such as A549 xenografts, while kinase-dead mutants of SIK3 can enhance tumor growth.

Other names

SIK3 activatorSIK-3 activatorSIK 3 activator