Literature DB >> 25589934

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

Nis Halland1, Friedemann Schmidt1, Tilo Weiss1, Joachim Saas1, Ziyu Li1, Jörg Czech1, Matthias Dreyer1, Armin Hofmeister1, Katharina Mertsch1, Uwe Dietz1, Carsten Strübing1, Marc Nazare2.   

Abstract

From a virtual screening starting point, inhibitors of the serum and glucocorticoid regulated kinase 1 were developed through a combination of classical medicinal chemistry and library approaches. This resulted in highly active small molecules with nanomolar activity and a good overall in vitro and ADME profile. Furthermore, the compounds exhibited unusually high kinase and off-target selectivity due to their rigid structure.

Entities:  

Keywords:  AGC kinase; Serum glucocorticoid regulated kinase; WNT signaling; virtual screening

Year:  2014        PMID： 25589934      PMCID： PMC4291729          DOI： 10.1021/ml5003376

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  27 in total

1.  Assessing the performance of OMEGA with respect to retrieving bioactive conformations.

Authors:  Jonas Boström; Jeremy R Greenwood; Johan Gottfries
Journal:  J Mol Graph Model       Date:  2003-03       Impact factor: 2.518

2.  How to optimize shape-based virtual screening: choosing the right query and including chemical information.

Authors:  Johannes Kirchmair; Simona Distinto; Patrick Markt; Daniela Schuster; Gudrun M Spitzer; Klaus R Liedl; Gerhard Wolber
Journal:  J Chem Inf Model       Date:  2009-03       Impact factor: 4.956

3.  Comparison of structure- and ligand-based virtual screening protocols considering hit list complementarity and enrichment factors.

Authors:  Dennis M Krüger; Andreas Evers
Journal:  ChemMedChem       Date:  2010-01       Impact factor: 3.466

4.  Stimulation of Na+/K+ ATPase activity and Na+ coupled glucose transport by β-catenin.

Authors:  Mentor Sopjani; Ioana Alesutan; Jan Wilmes; Miribane Dërmaku-Sopjani; Rebecca S Lam; Evgenia Koutsouki; Muharrem Jakupi; Michael Föller; Florian Lang
Journal:  Biochem Biophys Res Commun       Date:  2010-10-14       Impact factor: 3.575

5.  mTOR-raptor binds and activates SGK1 to regulate p27 phosphorylation.

Authors:  Feng Hong; Michelle D Larrea; Cheryl Doughty; David J Kwiatkowski; Rachel Squillace; Joyce M Slingerland
Journal:  Mol Cell       Date:  2008-06-20       Impact factor: 17.970

6.  The serum- and glucocorticoid-inducible kinase Sgk-1 is involved in pulmonary vascular remodeling: role in redox-sensitive regulation of tissue factor by thrombin.

Authors:  Rachida S BelAiba; Talija Djordjevic; Steve Bonello; Ferruh Artunc; Florian Lang; John Hess; Agnes Görlach
Journal:  Circ Res       Date:  2006-02-16       Impact factor: 17.367

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

Authors:  Francesco Ortuso; 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
Journal:  J Chem Inf Model       Date:  2014-06-13       Impact factor: 4.956

Review 8.  The physiological impact of the serum and glucocorticoid-inducible kinase SGK1.

Authors:  Florian Lang; Ferruh Artunc; Volker Vallon
Journal:  Curr Opin Nephrol Hypertens       Date:  2009-09       Impact factor: 2.894

9.  Identification of a novel serum and glucocorticoid regulated kinase-1 (SGK1) ligand from virtual screening.

Authors:  Werner J Geldenhuys; Phani K Talasila; Prabodh Sadana
Journal:  Bioorg Med Chem Lett       Date:  2012-07-15       Impact factor: 2.823

10.  PKB/SGK-resistant GSK-3 signaling following unilateral ureteral obstruction.

Authors:  Jakob Voelkl; Sobuj Mia; Adrian Meissner; Mohamed S Ahmed; Martina Feger; Bernat Elvira; Britta Walker; Dario R Alessi; Ioana Alesutan; Florian Lang
Journal:  Kidney Blood Press Res       Date:  2014-03-15       Impact factor: 2.687
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  18 in total

Review 1.  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

Review 2.  SGK1: The Dark Side of PI3K Signaling.

Authors:  Antonio Di Cristofano
Journal:  Curr Top Dev Biol       Date:  2016-12-15       Impact factor: 4.897

3.  mTORC2 Regulates Amino Acid Metabolism in Cancer by Phosphorylation of the Cystine-Glutamate Antiporter xCT.

Authors:  Yuchao Gu; Claudio P Albuquerque; Daniel Braas; Wei Zhang; Genaro R Villa; Junfeng Bi; Shiro Ikegami; Kenta Masui; Beatrice Gini; Huijun Yang; Timothy C Gahman; Andrew K Shiau; Timothy F Cloughesy; Heather R Christofk; Huilin Zhou; Kun-Liang Guan; Paul S Mischel
Journal:  Mol Cell       Date:  2017-06-22       Impact factor: 17.970

4.  Ontogeny and Vulnerabilities of Drug-Tolerant Persisters in HER2+ Breast Cancer.

Authors:  Chewei Anderson Chang; Jayu Jen; Shaowen Jiang; Azin Sayad; Arvind Singh Mer; Kevin R Brown; Allison M L Nixon; Avantika Dhabaria; Kwan Ho Tang; David Venet; Christos Sotiriou; Jiehui Deng; Kwok-Kin Wong; Sylvia Adams; Peter Meyn; Adriana Heguy; Jane A Skok; Aristotelis Tsirigos; Beatrix Ueberheide; Jason Moffat; Abhyudai Singh; Benjamin Haibe-Kains; Alireza Khodadadi-Jamayran; Benjamin G Neel
Journal:  Cancer Discov       Date:  2022-04-01       Impact factor: 38.272

5.  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

Review 6.  PROTACs to address the challenges facing small molecule inhibitors.

Authors:  Pedro Martín-Acosta; Xiangshu Xiao
Journal:  Eur J Med Chem       Date:  2020-11-05       Impact factor: 6.514

7.  Serum- and glucocorticoid-inducible kinase 1 activity in ventral tegmental area dopamine neurons regulates cocaine conditioned place preference but not cocaine self-administration.

Authors:  Marie A Doyle; Vedrana Bali; Andrew L Eagle; Ali R Stark; Barbara Fallon; Rachael L Neve; A J Robison; Michelle S Mazei-Robison
Journal:  Neuropsychopharmacology       Date:  2021-05-18       Impact factor: 8.294

8.  Modulation of the antibiotic activity against multidrug resistant strains of 4-(phenylsulfonyl) morpholine.

Authors:  Maria T A Oliveira; Alexandre M R Teixeira; Cícera J M Cassiano; Diniz M Sena; Henrique D M Coutinho; Irwin R A Menezes; Fernando G Figueredo; Luiz E Silva; Thiago A Toledo; Ricardo R F Bento
Journal:  Saudi J Biol Sci       Date:  2015-02-10       Impact factor: 4.219

9.  The hVps34-SGK3 pathway alleviates sustained PI3K/Akt inhibition by stimulating mTORC1 and tumour growth.

Authors:  Ruzica Bago; Eeva Sommer; Pau Castel; Claire Crafter; Fiona P Bailey; Natalia Shpiro; José Baselga; Darren Cross; Patrick A Eyers; Dario R Alessi
Journal:  EMBO J       Date:  2016-08-01       Impact factor: 11.598

10.  PDK1-SGK1 Signaling Sustains AKT-Independent mTORC1 Activation and Confers Resistance to PI3Kα Inhibition.

Authors:  Pau Castel; Haley Ellis; Ruzica Bago; Eneda Toska; Pedram Razavi; F Javier Carmona; Srinivasaraghavan Kannan; Chandra S Verma; Maura Dickler; Sarat Chandarlapaty; Edi Brogi; Dario R Alessi; José Baselga; Maurizio Scaltriti
Journal:  Cancer Cell       Date:  2016-07-21       Impact factor: 31.743
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