Table 2.
Strategies targeting Eph receptors and ephrin ligands for cancer therapy
| Treatment | Target | Tumour | References |
|---|---|---|---|
| Inhibitors of Eph/ephrin interaction | |||
| EphA2-FC, EphA3-FC | ephrinA | Breast cancer Pancreatic cancer | 142,149,150 |
| EphB4-FC | EphB4 | Melanoma | 156 |
| Mab2H9 antagonistic antibody | EphB2 | Colorectal cancer | 157 |
| TNYL-RAW peptide | EphB4 | Breast cancer | 158 |
| SNEW peptide | EphB2 | Breast cancer | 158 |
| KYL, APY, VTM peptide | EphA4 | Angiogenesis | 159,161 |
| 2,5-dimethylpyrroly benzoic acid derivatives | EphA4 | Angiogenesis | 161 |
| Disalicylic Acid-furanyl derivative | EphA2 | Prostate cancer | 205 |
| Activators of Eph forward signalling | |||
| EA2,B233,3F2-WT antibody | EphA2 | Breast cancer | 162 |
| EA5 antibody | EphA2 | Ovarian cancer | 163 |
| mAB208 | EphA2 | Renal cell cancer | 164 |
| Dimerized IIIA4 antibody | EphA3 | Malignant Melanoma | 183 |
| YSA, SWL peptides | EphA2 | Breast cancer | 206 |
| Kinase inhibitor | |||
| Dasatinib | EphA2 | Prostate cancer Ovarian cancer Pancreatic caner | 15,173,207 |
| Benzenesulphonamide derivative | EphB4 | Angiogenesis | 165 |
| Xanthine derivatives | EphB4 | Hepatocellular cancer | 168 |
| Inhibitor of Eph expression | |||
| EphA2 siRNA | EphA2 | Pancreatic cancer Ovarian cancer | 174 176,177 |
| EphB4 siRNA | EphB4 | Breast cancer | 100 |
| Oligonucleotides | EphB4 | Breast cancer Bladder cancer | 100,208 |
| Imaging agent | |||
| 64CU –DOTA-1C1 antibody | EphA2 | Colorectal cancer, Prostate cancer, Ovarian cancer, Glioblastoma, Malignant Melanoma | 182 |
| 111Indium-labelled IIIA4 antibody | EphA3 | Malignant Melanoma | 183 |
| Antibody-Drug/toxin conjugation | |||
| ephrinA1-PE38QQR | EphA2 | Glioblastoma | 13 |
| 1C1-maleimidocaproyl-MMAF conjugate | EphA2 | Prostate cancer | 179 |
| 2H9 antibody-vc-MMAE conjugate | EphB2 | Colorectal cancer | 157 |
| Immunotherapy | |||
| bscEphA2 × CD3 bispecific single-chain antibody | EphA2/CD3 | Breast cancer Colorectal cancer | 184 |
| EphA2-DCs | EphA2 | Colon cancer | 187 |
| EphA2833–891 peptide | EphA2 | Malignant gliomas | 14 |
| EphA3- and EphB6-derived peptides | EphA3/EphB6 | Glioma | 188,189 |