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EnglishThe activity of a series of imidazo[2,1-b]thiazole guanylhydrazones as inhibitors of p90 ribosomal S6 kinase 2 (RSK2) is described. It was found that a small subset of compounds show both potent inhibition of RSK2 kinase activity and tumor cell growth in vitro. Detailed study of one of the most active compounds indicates a high degree of selectivity for inhibition of RSK2 compared to a spectrum of other related kinases. Selective inhibition of the MCF-7 breast tumor cell line compared to MCF-10A nontransformed cells, as well as selective inhibition of the biomarker GSK3 provides evidence that the compounds can affect the RSK2 target in cells.
| Titolo: | Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors | |
| Autore/i: | ANDREANI, ALDO; GRANAIOLA, MASSIMILIANO; LEONI, ALBERTO; LOCATELLI, ALESSANDRA; MORIGI, RITA; RAMBALDI, MIRELLA; VAROLI, LUCILLA; D. Lannigan; J. Smith; D. Scudiero; S. Kondapaka; R. H. Shoemaker | |
| Autore/i Unibo: | ||
| Anno: | 2011 | |
| Rivista: | ||
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1016/j.ejmech.2011.07.001 | |
| Abstract: | The activity of a series of imidazo[2,1-b]thiazole guanylhydrazones as inhibitors of p90 ribosomal S6 kinase 2 (RSK2) is described. It was found that a small subset of compounds show both potent inhibition of RSK2 kinase activity and tumor cell growth in vitro. Detailed study of one of the most active compounds indicates a high degree of selectivity for inhibition of RSK2 compared to a spectrum of other related kinases. Selective inhibition of the MCF-7 breast tumor cell line compared to MCF-10A nontransformed cells, as well as selective inhibition of the biomarker GSK3 provides evidence that the compounds can affect the RSK2 target in cells. | |
| Data prodotto definitivo in UGOV: | 2013-06-26 16:22:28 | |
| Appare nelle tipologie: | 1.01 Articolo in rivista |
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