Table 1 The potential drugs targeting Hippo pathway in preclinical trials
From: The Hippo signalling pathway and its implications in human health and diseases
Mechanism | Drugs | Structure/sequence | Indications | |
|---|---|---|---|---|
YAP/TAZ nucleus/cytoplasm location | MSTs kinase activity inhibition | XMU-MP-1 |
| Chronic and acute liver injury Protest cancer Breast cancer Autoimmune encephalomyelitis Cardiac hypertrophy |
SBP-3264 |
| Acute myeloid leukaemia | ||
MSTs kinase expression inhibition | MST1/2-siRNA | MST1 (5’–3’ sense GAGUGUCAAUAUUGCGAGAtt) MST2 (5’–3’ sense CAAGAGUCAUGAAAAUUGUtt) | Deficiency of liver regeneration | |
LATs kinase activity inhibition | TRULI |
| No certain indication so far | |
Sav kinase expression inhibition | Sav-shRNA | Not post | Myocardial infarction Ischaemic heart failure | |
YAP-TEAD transcriptional activity regulation | YAP/TAZ expression inhibition | CA3 |
| Oesophageal adenocarcinoma Osteosarcoma tumour |
YAP-siRNA | Not post | Glioblastoma Hepatocellular carcinoma Posterior segment neovascularization-related ocular diseases | ||
YAP-shRNA | Not post | Lung fibrosis | ||
YAP-TEAD interaction inhibition | verteporfin |
| Glioblastoma Breast cancer Hepatocellular carcinoma Renal interstitial fibrogenesis Glaucoma | |
VGLL4-mimiking peptide | SVDDHFAKSLGDTWLQIGGSGNPK- TANVPQTVPMRLRKLPDSFFKPPE | Gastric cancer Colorectal cancer | ||
TEAD palmitoylation inhibition | Flufenamic acid derivative |
| Glioblastoma (in vitro) | |
