Table 2.
Agents targeting the Hippo pathway in breast cancer.
| Target | Drugs | Major Mechanisms | References |
|---|---|---|---|
| Raf | ISIS 5132 | Hybridizes to c-Raf mRNA, stopping the inactivation of MST | [94,95,96] |
| F-actin | Latrunculin | Activates LATS through regulating F-actin polymerization | [98,99,100] |
| ROCK | Y27632 | Activates LATS through inhibition of ROCK | [101,102] |
| HMG-CoA | Statins | Activates MST/LATS activity through Rho GTPases | [103,104] |
| PLD | CAY10594, FIPI | Reduces the production of PA, which could directly bind to and disrupt LATS and NF2 | [105] |
| ILK | QLT0267 | Activates MST by inhibiting ILK | [106,107] |
| Yes | Dasatinib | Activates kinase activity of Yes to activate YAP | [108,109] |
| PKC | Auranofin | Inhibits YAP through AMOT by inhibiting PKC | [110,111,112] |
| CDK1 | Taxol | Inhibits TAZ/YAP activity by activating CDK1 | [87,113] |
| BRD4 | BAY1238097 | Interacts with TAZ/YAP and downregulates their transcriptional activities by inhibiting BRD4 | [114] |
| AMPK | Metformin | Inhibits YAP activity by activating AMPK | [115,116,117] |
| YAP | Verteporfin | Disrupts YAP-TEAD interaction | [57,118,119,120] |
| AMOT | XAV939 | Suppresses YAP-TEAD transcriptional activities by maintaining the stabilization of AMOT | [124,125] |
| VEGFR & PDGFR | Pazopanib | Inhibits TAZ/YAP nuclear localization by inhibiting VEGFR and PDGFR | [127] |
| YAP | Cyclic Peptides | Peptides disrupting YAP-TEAD interaction | [128] |