Table 3.
Preclinical studies of TGF-β inhibitors for cancer treatment.
| Agents | Target | Experiments/Models | References |
|---|---|---|---|
| 1. THE LIGAND LEVEL | |||
| Trabedersen (AP12009) | TGF-β2 mRNA | In vivo: patient-derived gliomas | (119) |
| In vivo: induced melanoma tumor in mice | (120) | ||
| In vitro: pancreatic carcinomas | (121) | ||
| In vivo: human metastatic pancreatic cancer | (122) | ||
| In vivo: human colon carcinomas | (123) | ||
| 2. THE LIGAND-RECEPTOR LEVEL | |||
| Soluble TβRII | TβRII | In vitro: human metastatic pancreatic cancer cells | (124) |
| In vivo: patient-derived endometrial cancer | (125) | ||
| Soluble TβRIII (βglycan) | TβRIII | In vivo: patient-derived tissue from renal cancer | (126) |
| In vivo: patient-derived tissue non-small-cell lung carcinoma | (127) | ||
| In vivo: human xenograft model of breast cancer | (128) | ||
| 3. THE INTRACELLULAR LEVEL | |||
| Galunisertib (LY2157299) | TβRI | In vivo: patient-derived pancreatic, lung, colorectal cancer | (129) |
| In vivo: human ovarian cancer in nude mice | (130) | ||
| In vitro: hepatocellular carcinoma cells | (131–133) | ||
| Vactosertib (EW-7197) | TβRI | In vivo: lung metastases from breast cancer mice or transgenic MMTV/cNeu mice | (134) |
| EW-7195 | TβRI | In vivo: lung metastases from breast cancer mice | (135) |
| LY2109761 | TβRI/II | In vivo: metastatic colorectal cancer | (136) |
| In vivo: metastatic hepatocellular carcinoma | (137) | ||
| SD208 | TβRI | In vivo: metastatic breast cancer | (138) |
| In vivo: metastatic pancreatic cancer | (139) | ||