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, DORITData Curation
;Vighi, EleonoraData Curation
;Bertolotti, EvelinaData Curation
;Comitato, AntonellaData 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.File | Dimensione | Formato | |
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