Data di Pubblicazione:
2017
Citazione:
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]
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.
Tipologia CRIS:
Articolo su rivista
Keywords:
Caco-2; cGMP; HCT 116; HT-29; PKG2; VASP; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Proliferation; Cell Survival; Cyclic GMP; Dimerization; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Molecular Structure; Structure-Activity Relationship; Pharmacology; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry
Elenco autori:
Hoffmann, Dorit; Rentsch, Andreas; Vighi, Eleonora; Bertolotti, Evelina; Comitato, Antonella; Schwede, Frank; Genieser, Hans-Gottfried; Marigo, Valeria
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