Literature DB >> 24896223

In silico identification and biological evaluation of novel selective serum/glucocorticoid-inducible kinase 1 inhibitors based on the pyrazolo-pyrimidine scaffold.

Francesco Ortuso1, Rosario Amato, Anna Artese, Lucia D'antona, Giosuè Costa, Cristina Talarico, Francesco Gigliotti, Cataldo Bianco, Francesco Trapasso, Silvia Schenone, Francesca Musumeci, Lorenzo Botta, Nicola Perrotti, Stefano Alcaro.   

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 RAC-alpha serine/threonine-protein kinase (Akt1).

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Year:  2014        PMID： 24896223     DOI： 10.1021/ci500235f

Source DB:  PubMed          Journal:  J Chem Inf Model        ISSN： 1549-9596            Impact factor:   4.956


  18 in total

1.  Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors.

Authors:  Nis Halland; Friedemann Schmidt; Tilo Weiss; Joachim Saas; Ziyu Li; Jörg Czech; Matthias Dreyer; Armin Hofmeister; Katharina Mertsch; Uwe Dietz; Carsten Strübing; Marc Nazare
Journal:  ACS Med Chem Lett       Date:  2014-10-23       Impact factor: 4.345

Review 2.  PI3K signaling in cancer: beyond AKT.

Authors:  Evan C Lien; Christian C Dibble; Alex Toker
Journal:  Curr Opin Cell Biol       Date:  2017-03-24       Impact factor: 8.382

3.  Development of Pyrazolo[3,4-d]pyrimidine Kinase Inhibitors as Potential Clinical Candidates for Glioblastoma Multiforme.

Authors:  Chiara Greco; Vincenzo Taresco; Amanda K Pearce; Catherine E Vasey; Stuart Smith; Ruman Rahman; Cameron Alexander; Robert J Cavanagh; Francesca Musumeci; Silvia Schenone
Journal:  ACS Med Chem Lett       Date:  2020-02-13       Impact factor: 4.345

4.  Identification, structure modification, and characterization of potential small-molecule SGK3 inhibitors with novel scaffolds.

Authors:  Grace Qun Gong; Ke Wang; Xin-Chuan Dai; Yan Zhou; Rajesh Basnet; Yi Chen; De-Hua Yang; Woo-Jeong Lee; Christina Maree Buchanan; Jack Urquhart Flanagan; Peter Robin Shepherd; Ying Chen; Ming-Wei Wang
Journal:  Acta Pharmacol Sin       Date:  2018-07-23       Impact factor: 6.150

5.  Plasmin-Binding Tripeptide-Decorated Liposomes Loading Pyrazolo[3,4-d]pyrimidines for Targeting Hepatocellular Carcinoma.

Authors:  Pierpaolo Calandro; Giulia Iovenitti; Claudio Zamperini; Francesca Candita; Elena Dreassi; Mario Chiariello; Adriano Angelucci; Silvia Schenone; Maurizio Botta; Arianna Mancini
Journal:  ACS Med Chem Lett       Date:  2018-05-07       Impact factor: 4.345

6.  Water Solubility Enhancement of Pyrazolo[3,4-d]pyrimidine Derivatives via Miniaturized Polymer-Drug Microarrays.

Authors:  Monica Sanna; Giovanna Sicilia; Ali Alazzo; Nishant Singh; Francesca Musumeci; Silvia Schenone; Keith A Spriggs; Jonathan C Burley; Martin C Garnett; Vincenzo Taresco; Cameron Alexander
Journal:  ACS Med Chem Lett       Date:  2018-01-29       Impact factor: 4.345

7.  Preclinical model in HCC: the SGK1 kinase inhibitor SI113 blocks tumor progression in vitro and in vivo and synergizes with radiotherapy.

Authors:  Cristina Talarico; Lucia D'Antona; Domenica Scumaci; Agnese Barone; Francesco Gigliotti; Claudia Vincenza Fiumara; Vincenzo Dattilo; Enzo Gallo; Paolo Visca; Francesco Ortuso; Claudia Abbruzzese; Lorenzo Botta; Silvia Schenone; Giovanni Cuda; Stefano Alcaro; Cataldo Bianco; Patrizia Lavia; Marco G Paggi; Nicola Perrotti; Rosario Amato
Journal:  Oncotarget       Date:  2015-11-10

8.  SI113, a SGK1 inhibitor, potentiates the effects of radiotherapy, modulates the response to oxidative stress and induces cytotoxic autophagy in human glioblastoma multiforme cells.

Authors:  Cristina Talarico; Vincenzo Dattilo; Lucia D'Antona; Agnese Barone; Nicola Amodio; Stefania Belviso; Francesca Musumeci; Claudia Abbruzzese; Cataldo Bianco; Francesco Trapasso; Silvia Schenone; Stefano Alcaro; Francesco Ortuso; Tullio Florio; Marco G Paggi; Nicola Perrotti; Rosario Amato
Journal:  Oncotarget       Date:  2016-03-29

9.  JNK, p38, ERK, and SGK1 Inhibitors in Cancer.

Authors:  Jonas Cicenas; Egle Zalyte; Arnas Rimkus; Dalius Dapkus; Remigijus Noreika; Sigitas Urbonavicius
Journal:  Cancers (Basel)       Date:  2017-12-21       Impact factor: 6.639

10.  SGK1 affects RAN/RANBP1/RANGAP1 via SP1 to play a critical role in pre-miRNA nuclear export: a new route of epigenomic regulation.

Authors:  Vincenzo Dattilo; Lucia D'Antona; Cristina Talarico; Mjriam Capula; Giada Catalogna; Rodolfo Iuliano; Silvia Schenone; Sante Roperto; Cataldo Bianco; Nicola Perrotti; Rosario Amato
Journal:  Sci Rep       Date:  2017-03-30       Impact factor: 4.379
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