PMID- 26429069 OWN - NLM STAT- MEDLINE DCOM- 20160629 LR - 20220408 IS - 1875-533X (Electronic) IS - 0929-8673 (Linking) VI - 22 IP - 35 DP - 2015 TI - Targeting the Hippo Pathway for Anti-cancer Therapies. PG - 4104-17 AB - 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. FAU - Gong, Rui AU - Gong R FAU - Yu, Fa-Xing AU - Yu FX AD - Children's Hospital and Institutes of Biomedical Sciences, Fudan University, Shanghai 200032, China. fxyu@fudan.edu.cn. LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PT - Review PL - United Arab Emirates TA - Curr Med Chem JT - Current medicinal chemistry JID - 9440157 RN - 0 (Antineoplastic Agents) RN - 0 (Small Molecule Libraries) RN - EC 2.7.11.1 (Protein Serine-Threonine Kinases) SB - IM MH - Antineoplastic Agents/*pharmacology MH - Hippo Signaling Pathway MH - Humans MH - Models, Molecular MH - Molecular Structure MH - Protein Serine-Threonine Kinases/*antagonists & inhibitors/metabolism MH - Signal Transduction/*drug effects MH - Small Molecule Libraries/*pharmacology MH - Structure-Activity Relationship EDAT- 2015/10/03 06:00 MHDA- 2016/06/30 06:00 CRDT- 2015/10/03 06:00 PHST- 2015/09/22 00:00 [received] PHST- 2015/09/28 00:00 [revised] PHST- 2015/09/29 00:00 [accepted] PHST- 2015/10/03 06:00 [entrez] PHST- 2015/10/03 06:00 [pubmed] PHST- 2016/06/30 06:00 [medline] AID - CMC-EPUB-70833 [pii] AID - 10.2174/0929867322666151002112256 [doi] PST - ppublish SO - Curr Med Chem. 2015;22(35):4104-17. doi: 10.2174/0929867322666151002112256.