The Hippo pathway is an important organ size control signaling network and the 
major regulatory mechanism of cell-contact inhibition. Yes associated protein 
(YAP) and transcriptional co-activator with PDZ-binding motif (TAZ) are its 
targets and terminal effectors: inhibition of the pathway promotes YAP/TAZ 
translocation to the nucleus, where they interact with transcriptional enhancer 
associate domain (TEAD) transcription factors and coactivate the expression of 
target genes, promoting cell proliferation. Defects in the pathway can result in 
overgrowth phenotypes due to deregulation of stem-cell proliferation and 
apoptosis; members of the pathway are directly involved in cancer development. 
The pharmacological regulation of the pathway might be useful in cancer 
prevention, treatment, and regenerative medicine applications; currently, a few 
compounds can selectively modulate the pathway. In this review, we present an 
overview of the Hippo pathway, the sequence and structural analysis of YAP/TAZ, 
the known pharmacological modulators of the pathway, especially those targeting 
YAP/TAZ-TEAD interaction.