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Table 1 Summary of EphA2 targeted therapies against cancer

From: Targeting EphA2 in cancer

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   [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  
  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  
  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]