LKB1 is a serine/threonine kinase that belongs to the AMPK-related kinase family. LKB1 functions as a heterotrimeric complex with STRAD (STE20-related adaptor) and MO25 (mouse protein 25) proteins, which are necessary for its stability and full kinase activity. LKB1 is mutated in a variety of cancers, including Peutz-Jeghers syndrome (PJS), a rare autosomal dominant disorder characterized by benign gastrointestinal polyps and increased risk of malignancies. Inactivation of LKB1 leads to enhanced cell proliferation, altered energy metabolism, and resistance to apoptosis, promoting tumor development. Restoring LKB1 function has been shown to suppress tumor growth and metastasis in various cancer models. LKB1 is also a master kinase that activates multiple downstream kinases involved in cellular energy metabolism, including AMP-activated protein kinase (AMPK) and 12 related kinases (MARKs).