The CXCR4 Antagonist R54 Targets Epithelial-Mesenchymal Transition (EMT) in Human Ovarian Cancer Cells

Creators

• Russo Daniela
• Spina Anna
• Portella Luigi
• Bello Anna Maria
• Galdiero Francesca
• Trotta Anna Maria
• Ieranò Caterina
• Rea Giuseppina
• Cecere Sabrina Chiara
• Coppola Elisabetta
• Di Maro Salvatore
• Pignata Sandro
• Califano Daniela
• Scala Stefania

Description

Abstract

The axis CXCL12-CXCR4 is highly expressed in ovarian cancer where it contributes to disease progression. The aim of this work was to evaluate the effect of the newly developed CXCR4 antagonist R54 on human ovarian cancer cell aggressiveness.

The CXCL12-CXCR4 axis was assessed in human ovarian cancer cells through:
- Proliferation
- Migration
- CXCL12-dependent signaling

Epithelial-to-mesenchymal transition (EMT) was analyzed via markers:
- E-CADHERIN
- N-CADHERIN
- VIMENTIN
- SNAIL1
- ΒETA-CATENIN

Methods used include:
- qRT-PCR
- Immunofluorescence
- Immunoblotting

Key Findings:
- R54 inhibited CXCL12-induced proliferation and migration of ovarian cancer cells.
- R54 suppressed CXCL12-dependent pERK1/2 and pAKT signaling.
- R54 reversed CXCL12-induced EMT, reducing mesenchymal traits in ovarian cancer cells.

Conclusion:
Targeting CXCR4 with the antagonist R54 effectively reverted EMT in human ovarian cancer cells, diminishing their migratory and chemoresistance features.