Activation of the cGMP-dependent protein kinase G (PKG) can inhibit growth and/or induce apoptosis in colon cancer. In this study we evaluated the effects on cell viability, cell death and proliferation of novel dimeric cGMP analogues, compared to a monomeric compound. Three colon cancer cell lines, which only express isoform 2 of PKG, were treated with these novel cGMP analogues and responded with increased PKG activity. cGMP analogues reduced cell viability in the three cell lines and this was due to a cytostatic rather than cytotoxic effect. These findings suggest that activation of PKG2 can be a therapeutic target in the treatment of colon cancer and, most importantly, that dimeric cGMP analogues can further improve the beneficial effects previously observed with monomeric cGMP analogues.

New dimeric cGMP analogues reduce proliferation in three colon cancer cell lines / Hoffmann, Dorit; Rentsch, Andreas; Vighi, Eleonora; Bertolotti, Evelina; Comitato, Antonella; Schwede, Frank; Genieser, Hans-Gottfried; Marigo, Valeria. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 141:(2017), pp. 61-72. [10.1016/j.ejmech.2017.09.053]

New dimeric cGMP analogues reduce proliferation in three colon cancer cell lines

HOFFMANN, DORIT
Data Curation
;
Vighi, Eleonora
Data Curation
;
Bertolotti, Evelina
Data Curation
;
Comitato, Antonella
Data Curation
;
Marigo, Valeria
2017

Abstract

Activation of the cGMP-dependent protein kinase G (PKG) can inhibit growth and/or induce apoptosis in colon cancer. In this study we evaluated the effects on cell viability, cell death and proliferation of novel dimeric cGMP analogues, compared to a monomeric compound. Three colon cancer cell lines, which only express isoform 2 of PKG, were treated with these novel cGMP analogues and responded with increased PKG activity. cGMP analogues reduced cell viability in the three cell lines and this was due to a cytostatic rather than cytotoxic effect. These findings suggest that activation of PKG2 can be a therapeutic target in the treatment of colon cancer and, most importantly, that dimeric cGMP analogues can further improve the beneficial effects previously observed with monomeric cGMP analogues.
2017
27-set-2017
141
61
72
New dimeric cGMP analogues reduce proliferation in three colon cancer cell lines / Hoffmann, Dorit; Rentsch, Andreas; Vighi, Eleonora; Bertolotti, Evelina; Comitato, Antonella; Schwede, Frank; Genieser, Hans-Gottfried; Marigo, Valeria. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 141:(2017), pp. 61-72. [10.1016/j.ejmech.2017.09.053]
Hoffmann, Dorit; Rentsch, Andreas; Vighi, Eleonora; Bertolotti, Evelina; Comitato, Antonella; Schwede, Frank; Genieser, Hans-Gottfried; Marigo, Valeria
File in questo prodotto:
File Dimensione Formato  
EJMECH-D-17-00438R1.pdf

Open Access dal 29/09/2019

Tipologia: Versione dell'autore revisionata e accettata per la pubblicazione
Dimensione 804.82 kB
Formato Adobe PDF
804.82 kB Adobe PDF Visualizza/Apri
Pubblicazioni consigliate

Licenza Creative Commons
I metadati presenti in IRIS UNIMORE sono rilasciati con licenza Creative Commons CC0 1.0 Universal, mentre i file delle pubblicazioni sono rilasciati con licenza Attribuzione 4.0 Internazionale (CC BY 4.0), salvo diversa indicazione.
In caso di violazione di copyright, contattare Supporto Iris

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11380/1151591
Citazioni
  • ???jsp.display-item.citation.pmc??? 5
  • Scopus 11
  • ???jsp.display-item.citation.isi??? 11
social impact