Literature DB >> 25738750

Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.

Jason G Kettle1, Peter Ballard1, Catherine Bardelle1, Mark Cockerill1, Nicola Colclough1, Susan E Critchlow1, Judit Debreczeni1, Gary Fairley1, Shaun Fillery1, Mark A Graham1, Louise Goodwin1, Sylvie Guichard1, Kevin Hudson1, Richard A Ward1, David Whittaker1.   

Abstract

Potent and selective inhibitors of Dyrk1B kinase were developed to explore the hypothesis, based on siRNA studies, that Dyrk1B may be a resistance mechanism in cells undergoing a stress response.

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Year:  2015        PMID: 25738750     DOI: 10.1021/acs.jmedchem.5b00098

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  4 in total

1.  Novel and Potential Small Molecule Scaffolds as DYRK1A Inhibitors by Integrated Molecular Docking-Based Virtual Screening and Dynamics Simulation Study.

Authors:  Mir Mohammad Shahroz; Hemant Kumar Sharma; Abdulmalik S A Altamimi; Mubarak A Alamri; Abuzer Ali; Amena Ali; Safar Alqahtani; Ali Altharawi; Alhumaidi B Alabbas; Manal A Alossaimi; Yassine Riadi; Ahmad Firoz; Obaid Afzal
Journal:  Molecules       Date:  2022-02-09       Impact factor: 4.411

2.  In vivo drug discovery for increasing incretin-expressing cells identifies DYRK inhibitors that reinforce the enteroendocrine system.

Authors:  Lianhe Chu; Michishige Terasaki; Charlotte L Mattsson; Romain Teinturier; Jérémie Charbord; Ercument Dirice; Ka-Cheuk Liu; Michael G Miskelly; Qiao Zhou; Nils Wierup; Rohit N Kulkarni; Olov Andersson
Journal:  Cell Chem Biol       Date:  2022-08-22       Impact factor: 9.039

3.  Exploring Ligand Stability in Protein Crystal Structures Using Binding Pose Metadynamics.

Authors:  Lucia Fusani; David S Palmer; Don O Somers; Ian D Wall
Journal:  J Chem Inf Model       Date:  2020-01-22       Impact factor: 4.956

Review 4.  Minibrain-related kinase/dual-specificity tyrosine-regulated kinase 1B implication in stem/cancer stem cells biology.

Authors:  Nikolaos Kokkorakis; Maria Gaitanou
Journal:  World J Stem Cells       Date:  2020-12-26       Impact factor: 5.326

  4 in total

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