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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Targeting the Hippo Pathway for Anti-cancer Therapies

Author(s): Rui Gong and Fa-Xing Yu

Volume 22, Issue 35, 2015

Page: [4104 - 4117] Pages: 14

DOI: 10.2174/0929867322666151002112256

Price: $65


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.

Keywords: Hippo, TAZ, TEAD, Verteporfin, VGLL4, YAP.

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