The CXCR4 antagonist R54 targets epithelial-mesenchymal transition (EMT) in human ovarian cancer cells.

The axis CXCL12-CXCR4 is highly expressed in ovarian cancer where contributes to disease progression. Aim of the work was to evaluate the effect of the newly developed CXCR4 antagonist R54 on human ovarian cancer cells aggressiveness. CXCL12-CXCR4 axis was evaluated in human ovarian cancer cells thr...

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Main Authors: Daniela Russo, Anna Spina, Luigi Portella, Anna Maria Bello, Francesca Galdiero, Anna Maria Trotta, Caterina Ieranò, Giuseppina Rea, Sabrina Chiara Cecere, Elisabetta Coppola, Salvatore Di Maro, Sandro Pignata, Daniela Califano, Stefania Scala
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2024-01-01
Series:PLoS ONE
Online Access:https://doi.org/10.1371/journal.pone.0314735
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author Daniela Russo
Anna Spina
Luigi Portella
Anna Maria Bello
Francesca Galdiero
Anna Maria Trotta
Caterina Ieranò
Giuseppina Rea
Sabrina Chiara Cecere
Elisabetta Coppola
Salvatore Di Maro
Sandro Pignata
Daniela Califano
Stefania Scala
author_facet Daniela Russo
Anna Spina
Luigi Portella
Anna Maria Bello
Francesca Galdiero
Anna Maria Trotta
Caterina Ieranò
Giuseppina Rea
Sabrina Chiara Cecere
Elisabetta Coppola
Salvatore Di Maro
Sandro Pignata
Daniela Califano
Stefania Scala
author_sort Daniela Russo
collection DOAJ
description The axis CXCL12-CXCR4 is highly expressed in ovarian cancer where contributes to disease progression. Aim of the work was to evaluate the effect of the newly developed CXCR4 antagonist R54 on human ovarian cancer cells aggressiveness. CXCL12-CXCR4 axis was evaluated in human ovarian cancer cells through proliferation, migration and signaling CXCL12-dependents. Epithelial to mesenchymal transition (EMT) was analyzed through E-CADHERIN, N-CADHERIN, VIMENTIN, SNAIL1 and ΒETA-CATENIN by qRT-PCR, immunofluorescence and immunoblotting. R54 inhibited ovarian cancer cells proliferation and migration CXCL12-induced. Moreover, R54 inhibited CXCL12 dependent pERK1/2 and pAKT and reversed the CXCL12 induced EMT in ovarian cancer cells. Targeting CXCR4 with the new antagonist R54 consistently reverted the mesenchymal transition in human ovarian cancer cells reducing migratory and chemoresistance features.
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spelling doaj-art-63d9516daf4840f3be1a6ca78a8fada42025-01-08T05:32:57ZengPublic Library of Science (PLoS)PLoS ONE1932-62032024-01-011912e031473510.1371/journal.pone.0314735The CXCR4 antagonist R54 targets epithelial-mesenchymal transition (EMT) in human ovarian cancer cells.Daniela RussoAnna SpinaLuigi PortellaAnna Maria BelloFrancesca GaldieroAnna Maria TrottaCaterina IeranòGiuseppina ReaSabrina Chiara CecereElisabetta CoppolaSalvatore Di MaroSandro PignataDaniela CalifanoStefania ScalaThe axis CXCL12-CXCR4 is highly expressed in ovarian cancer where contributes to disease progression. Aim of the work was to evaluate the effect of the newly developed CXCR4 antagonist R54 on human ovarian cancer cells aggressiveness. CXCL12-CXCR4 axis was evaluated in human ovarian cancer cells through proliferation, migration and signaling CXCL12-dependents. Epithelial to mesenchymal transition (EMT) was analyzed through E-CADHERIN, N-CADHERIN, VIMENTIN, SNAIL1 and ΒETA-CATENIN by qRT-PCR, immunofluorescence and immunoblotting. R54 inhibited ovarian cancer cells proliferation and migration CXCL12-induced. Moreover, R54 inhibited CXCL12 dependent pERK1/2 and pAKT and reversed the CXCL12 induced EMT in ovarian cancer cells. Targeting CXCR4 with the new antagonist R54 consistently reverted the mesenchymal transition in human ovarian cancer cells reducing migratory and chemoresistance features.https://doi.org/10.1371/journal.pone.0314735
spellingShingle Daniela Russo
Anna Spina
Luigi Portella
Anna Maria Bello
Francesca Galdiero
Anna Maria Trotta
Caterina Ieranò
Giuseppina Rea
Sabrina Chiara Cecere
Elisabetta Coppola
Salvatore Di Maro
Sandro Pignata
Daniela Califano
Stefania Scala
The CXCR4 antagonist R54 targets epithelial-mesenchymal transition (EMT) in human ovarian cancer cells.
PLoS ONE
title The CXCR4 antagonist R54 targets epithelial-mesenchymal transition (EMT) in human ovarian cancer cells.
title_full The CXCR4 antagonist R54 targets epithelial-mesenchymal transition (EMT) in human ovarian cancer cells.
title_fullStr The CXCR4 antagonist R54 targets epithelial-mesenchymal transition (EMT) in human ovarian cancer cells.
title_full_unstemmed The CXCR4 antagonist R54 targets epithelial-mesenchymal transition (EMT) in human ovarian cancer cells.
title_short The CXCR4 antagonist R54 targets epithelial-mesenchymal transition (EMT) in human ovarian cancer cells.
title_sort cxcr4 antagonist r54 targets epithelial mesenchymal transition emt in human ovarian cancer cells
url https://doi.org/10.1371/journal.pone.0314735
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