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Table 1 Summary of effects of small-molecule antagonists of the Tcf/β-catenin complex on endometriosis

From: Targeting the Wnt/β-catenin pathway in endometriosis: a potentially effective approach for treatment and prevention

Model

Cell type or species

Inhibitor

Parameters assessed

Functional effects

Reference

In vitro assay

C-EE, C-ES

PKF 115-584

Cell proliferation

C-EE, C-ES, E-EE, E-ES, EnE and EnS: significantly inhibited vs. non-treated cells

[4]

E-EE, E-ES

CGP049090

EnE, EnS

 

C-EE, C-ES

PKF 115-584

Cell migration

C-EE, C-ES, E-EE, E-ES, EnE and EnS: significantly inhibited vs. non-treated cells

[4]

E-EE, E-ES

EnE, EnS

 

C-EE, C-ES

PKF 115-584

Cell invasion

C-EE, C-ES, E-EE, E-ES, EnE and EnS: significantly inhibited vs. non treated cells

[4]

E-EE, E-ES

EnE, EnS

 

C-EE, C-ES

PKF 115-584

Tcf/β-catenin target genes (Cyclin D1, Survivin, c-Myc, MMP2, MMP9)

C-EE, C-ES, E-EE, E-ES, EnE and EnS: cyclin D1, Survivin, MMP2 and MMP9 mRNA: significantly decreased vs. non-treated cells

[4]

E-EE, E-ES

EnE, EnS

Total form of MMP-9 in E-EE or E-ES: significantly decreased vs. C-EE or C-ES

Active forms of MMP-2 in EnE: significantly decreased vs. E-EE

Total form of MMP-9 in EnS: significantly decreased vs. E-ES

 

E-ES, EnS

PKF 115-584

Fibrotic markers (αSMA, Col-I, CTGF, and FN)

E-ES, EnS: αSMA, Col-I, CTGF, and FN mRNA (with or without TGF ß1 stimulation): significantly decreased vs. non-treated cells

[4]

CGP049090

EnS: percentage of αSMA-positive cells: significantly decrased vs. non-treated cells

 
 

E-ES, EnS

PKF 115-584

Collagen gel contraction

E-ES, EnS: significantly decreased vs. non-treated cells

[5]

CGP049090

In vivo assay

Mouse (female Swiss nude mice)

CGP049090

Severity of fibrosis in endometriotic implants assessed by Sirius Red or Masson Trichrome stains

Staining scores for Sirius Red or Masson Trichrome stains: significantly lower vs. non-treated mice

[5]

  1. C-EE: endometrial epithelial cells of patients without endometriosis, C-ES: endometrial stromal cells of patients without endometriosis.
  2. E-EE: Endometrial epithelial cell of patients with endometriosis, E-ES: endometrial stromal cell of patients with endometriosis.
  3. EnE: Endometriotic epithelial cells, EnS: endometriotic stromal cells.
  4. MMP-2: Matrix metalloproteinase-2, MMP-9: Matrix metalloproteinase-9, αSMA: alpha smooth muscle actin, Col-I: Type I collagen.
  5. CTGF: connective tissue growth factor, FN: fibronection.