Regulation of the Hippo pathway and implications for anticancer drug development.
Research in the past decade has revealed key components of the Hippo tumor suppressor pathway and its critical role in organ size regulation and tumorigenesis. Recent progress has identified a wide range of upstream factors that control the Hippo pathway, which include cell-cell contact, various diffusible signals, and cognate receptors. Dysregulation of the Hippo pathway, caused by gene mutation or aberrant expression, promotes cell proliferation and tumorigenesis. Here, we discuss the current state of Hippo pathway research, primarily focusing on upstream regulators and protein-protein interactions as potential therapeutic targets. Consideration of pharmacological intervention of the Hippo pathway may provide novel avenues for future therapeutic treatment of human diseases, particularly in cancer.
Department of Pharmacology and Moores Cancer Center, University of California San Diego, La Jolla, CA 92093, USA.
Hyun Woo
HW
Park
Kun-Liang
KL
Guan
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D000090683:Hippo Signaling Pathway; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology*; D017346:Protein Serine-Threonine Kinases / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects
D000970:Antineoplastic Agents; D017346:Protein Serine-Threonine Kinases
GPCR; Hippo pathway; YAP; cancer; phosphorylation