Mechanism | Method or compound | Cancer type | Exact effects on EphA2 | Effects in vitro | Effects in vivo | Ref. |
---|---|---|---|---|---|---|
Decrease EphA2 expression | ||||||
 | EPHARNA | Ovarian cancer | Decrease in vivo EphA2 expression | – | Inhibit tumor growth | [49] |
Promote EphA2 degradation | ||||||
 | Soluble ephrin A1 and ephrin A1-Fc | |||||
Ephrin A1 | Glioblastoma multiforme | Induce EphA2 internalization and downregulation | Inhibit cell migration | Â | [50] | |
Monomeric ephrin A1 | Breast cancer | Induce EphA2 phosphorylation and degradation | – | – | [51] | |
Ephrin A1-Fc | Pancreatic cancer | Induce EphA2 degradation | Inhibit cell motility and invasion | – | [52] | |
Ephrin A1-Fc | Gastric cancer | Induce EphA2 phosphorylation and degradation | Inhibit cell growth | – | [53] | |
EphA2 monoclonal antibody | ||||||
EA1.2 | Breast cancer | Induce EphA2 phosphorylation and degradation | Inhibit cell growth, disrupt angiogenesis | – | [45] | |
EA2 and B233 | Breast cancer | Induce EphA2 phosphorylation and degradation | inhibit tumor growth in vivo | Inhibit tumor growth | [54] | |
D2 scFv | Lymphoma | Prevent EphA2-ephrin interaction | Inhibit cell proliferation, induce apoptosis | – | [55] | |
SHM16 | Melanoma | Antibody internalization | Inhibit cell migration and invasion | – | [43] | |
DS-8895a | Breast cancer and gastric cancer | Inhibit EphA2 phosphorylation | – | Inhibit tumor growth | [56] | |
DS-8895a | Breast cancer and gastric cancer | – | – | Inhibit tumor growth | [57] | |
3F2-3M | Breast, ovarian, non-small cell lung cancer | Induce EphA2 phosphorylation | Kill tumor cells in vitro | Inhibit tumor growth | [44] | |
Block endogenous EphA2 activation | ||||||
 | Inhibit Eph-ephrin interactions | |||||
EphA2-Fc | Pancreatic | Inhibit EphA2 phosphorylation | Inhibit angiogenesis | Inhibit tumor growth | [58] | |
Lithocholic acid | Prostate and colon cancer | Inhibit EphA2 phosphorylation | Inhibit cell rounding, retraction | – | [59] | |
UniPR126 | Prostate cancer | Inhibit EphA2 phosphorylation | Inhibit cell rounding, retraction | – | [60] | |
UniPR126 | Prostate cancer | Inhibit EphA2 phosphorylation | – | – | [61] | |
UniPR129 | Prostate cancer | Inhibit EphA2 phosphorylation and block kinase domain enzymatic activity | Inhibit cell rounding, disrupt angiogenesis | [62] | ||
UniPR1331 | Prostate cancer | block EphA2 phosphorylation and activation | Disrupt angiogenesis | – | [63] | |
Cholanic acid | Prostate cancer | Inhibit EphA2 phosphorylation | Inhibit cell retraction | – | [64] | |
GW4064 | Prostate cancer | Inhibit EphA2 phosphorylation | – | – | [65] | |
76D10 | Prostate cancer | Inhibit EphA2 phosphorylation | Inhibit cell retraction | – | [66] | |
Inhibit kinase activity of EphA2 | ||||||
Dasatinib | Melanoma | Inhibit EphA2 phosphorylation and kinase activity | Inhibit cell migration and invasion | – | [67] | |
Dasatinib | Pancreatic cancer | Inhibit EphA2 phosphorylation and kinase activity | Inhibit cell growth | – | [68] | |
Candidate 4a | Glioblastoma | – | Inhibit cell survival | – | [69] | |
ALW-II-41-27 | Non-small cell lung cancer | Inhibit EphA2 phosphorylation | Inhibit cell survival | Inhibit tumor growth | [70] | |
ALW-II-41-27 | Lung cancer | – | Inhibit cell survival, proliferation, migration, increased apoptosis | Inhibit tumor growth | [25] | |
EphA2 as drug delivery target | Â | |||||
 | Peptide/antibody-drug conjugates | |||||
Ephrin A1–PE38QQR | Glioblastoma multiforme | Decrease EphA2 expression | Inhibit cell survival | – | [71] | |
MEDI-547 | Prostate cancer | Induce EphA2 phosphorylation and degradation | Inhibit cell survival | Inhibit tumor growth | [72] | |
MEDI-547 | Endometrial cancer | Induce EphA2 internalization and degradation | Inhibit cell survival, induce apoptosis | Inhibit tumor growth | [73] | |
MEDI-547 | Ovarian cancer | Induce EphA2 degradation | Inhibit cell survival and proliferation, induce apoptosis | Inhibit tumor growth | [74] | |
Antibody-directed nanotherapeutics | ||||||
YTPL | Melanoma | – | Inhibit cell survival | – | [75] | |
MM-310 | Breast, prostate, gastric, and esophageal cancer | – | – | Inhibit tumor growth | [76] | |
EphA2-based immunotherapy | Â | |||||
 | DC-vaccine | Colon cancer (murine) | – | – | Inhibit tumor growth | [77] |
DC-vaccine | Colon cancer (murine) and melanoma (human) | – | – | Inhibit tumor growth | [78] | |
CAR T cells | Glioblastoma | Decrease EphA2 expression | – | Inhibit tumor growth | [79] | |
CAR T cells | Glioma | – | – | Inhibit tumor growth | [80] | |
CAR T cells | Lung cancer | – | Inhibit cell survival | Inhibit tumor growth | [81] | |
CAR T cells | Esophageal squamous cell carcinoma | – | Inhibit cell survival | – | [82] |