Targeting the Hippo Pathway and Cancer through the TEAD Family of Transcription Factors
AbstractThe Hippo pathway is a critical transcriptional signaling pathway that regulates cell growth, proliferation and organ development. The transcriptional enhanced associate domain (TEAD) protein family consists of four paralogous transcription factors that function to modulate gene expression in response to the Hippo signaling pathway. Transcriptional activation of these proteins occurs upon binding to the co-activator YAP/TAZ whose entry into the nucleus is regulated by Lats1/2 kinase. In recent years, it has become apparent that the dysregulation and/or overexpression of Hippo pathway effectors is implicated in a wide range of cancers, including prostate, gastric and liver cancer. A large body of work has been dedicated to understanding the therapeutic potential of modulating the phosphorylation and localization of YAP/TAZ. However, YAP/TAZ are considered to be natively unfolded and may be intractable as drug targets. Therefore, TEAD proteins present themselves as an excellent therapeutic target for intervention of the Hippo pathway. This review summarizes the functional role of TEAD proteins in cancer and assesses the therapeutic potential of antagonizing TEAD function in vivo. View Full-Text
Share & Cite This Article
Holden, J.K.; Cunningham, C.N. Targeting the Hippo Pathway and Cancer through the TEAD Family of Transcription Factors. Cancers 2018, 10, 81.
Holden JK, Cunningham CN. Targeting the Hippo Pathway and Cancer through the TEAD Family of Transcription Factors. Cancers. 2018; 10(3):81.Chicago/Turabian Style
Holden, Jeffrey K.; Cunningham, Christian N. 2018. "Targeting the Hippo Pathway and Cancer through the TEAD Family of Transcription Factors." Cancers 10, no. 3: 81.
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.