Hippo signaling pathway components

The Hippo signaling pathway is an evolutionarily conserved kinase cascade that regulates organ size, cell proliferation, apoptosis, tissue regeneration, and stem cell function. Its core components include kinases MST1/2 and LATS1/2, scaffold proteins SAV1 and MOB1A/B, and the transcriptional co-activators YAP and TAZ, which, when active, interact with TEAD1-4 transcription factors to drive gene expression changes. Dysregulation of the Hippo pathway is implicated in various diseases, most notably human cancers, where hyperactivation of YAP/TAZ leads to tumor growth, metastasis, and therapy resistance. The pathway is a prominent target for emerging cancer therapeutics, most of which aim to inhibit YAP/TAZ-TEAD function; examples include small molecules such as verteporfin. However, because the Hippo pathway comprises multiple proteins with diverse cellular roles, therapeutic targeting faces challenges including specificity, toxicity, and the need for biomarker-based patient selection

Other names

Hippo pathwayHippo signaling pathwayHippo-YAP pathwayMST1/2-LATS1/2-YAP/TAZ pathway

Inhibition of YAP/TAZ-TEAD protein-protein interaction; Prevention of YAP/TAZ nuclear localization; Inhibition of MST1/2 kinase activity; Blocking TEAD palmitoylation and/or DNA binding; Indirect modulation via upstream signaling (e.g., GPCRs, Wnt, TGF-β, cytoskeleton)