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American Chemical Society, Journal of Chemical Information and Modeling, 7(54), p. 1828-1832, 2014

DOI: 10.1021/ci500235f

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In Silico Identification and Biological Evaluation of Novel Selective Serum/Glucocorticoid-Inducible Kinase 1 Inhibitors Based on the Pyrazolo-Pyrimidine Scaffold

Journal article published in 2014 by Francesco Ortuso, Rosario Amato, Anna Artese, Lucia D'antona, Giosue Costa ORCID, Cristina Talarico, Francesco Gigliotti, Cataldo Bianco, Francesco Trapasso, Silvia Schenone, Francesca Musumeci ORCID, Lorenzo Botta, Nicola Perrotti, Stefano Alcaro
This paper is available in a repository.
This paper is available in a repository.

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Abstract

The Serum/Glucocorticoid-inducible kinase 1 (Sgk1) has demonstrated antiapoptotic function and the capability to regulate cell survival, proliferation and differentiation. A pivotal role of Sgk1 in carcinogenesis and in resistance to anticancer therapy has been suggested. With the aim of identifying new Sgk1 modulators, 322 pyrazolo-pyrimidine derivatives have been virtually screened with respect to a crystallographic model of Sgk1. The top five ranked compounds have been evaluated demonstrating Sgk1 inhibition in vitro and selectivity compared to Akt1.