The Hippo signaling pathway is critical in regulating tissue homeostasis, organ
size, and tumorigenesis. YAP and TAZ, two major effectors of the Hippo pathway, function
as transcriptional co-activators and promote target gene expression mainly through interaction
with TEAD family transcription factors. As oncoproteins, YAP and TAZ are frequently
activated or highly expressed in various cancer specimens. Moreover, their activity has been linked to resistance
to a few widely used anti-cancer drugs, and YAP activation contributes to cancer relapse. Thus, the
Hippo pathway, especially YAP/TAZ-TEAD interaction, represents an attractive target for anti-cancer therapies.
Here, we will discuss potential approaches to inhibit YAP/TAZ activity, and also review currently available
small molecules targeting the Hippo pathway.