Literature DB >> 21565500

Structure-based lead identification of ATP-competitive MK2 inhibitors.

Tjeerd Barf1, Allard Kaptein, Sander de Wilde, Ruud van der Heijden, Richard van Someren, Dennis Demont, Carsten Schultz-Fademrecht, Judith Versteegh, Mario van Zeeland, Nicole Seegers, Bert Kazemier, Bas van de Kar, Maaike van Hoek, Jeroen de Roos, Henri Klop, Ruben Smeets, Claudia Hofstra, Jorrit Hornberg, Arthur Oubrie.   

Abstract

MK2 kinase is a promising drug discovery target for the treatment of inflammatory diseases. Here, we describe the discovery of novel MK2 inhibitors using X-ray crystallography and structure-based drug design. The lead has in vivo efficacy in a short-term preclinical model.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21565500     DOI: 10.1016/j.bmcl.2011.04.018

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  8 in total

1.  Structure of the β-form of human MK2 in complex with the non-selective kinase inhibitor TEI-L03090.

Authors:  Aiko Fujino; Kei Fukushima; Takaharu Kubota; Yoshiyuki Matsumoto; Midori Takimoto-Kamimura
Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun       Date:  2013-11-28

2.  Certain ortho-hydroxylated brominated ethers are promiscuous kinase inhibitors that impair neuronal signaling and neurodevelopmental processes.

Authors:  Robert G Poston; Lillian Murphy; Ayna Rejepova; Mina Ghaninejad-Esfahani; Joshua Segales; Kimberly Mulligan; Ramendra N Saha
Journal:  J Biol Chem       Date:  2020-03-30       Impact factor: 5.157

Review 3.  Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials.

Authors:  Mario Fiore; Stefano Forli; Fabrizio Manetti
Journal:  J Med Chem       Date:  2015-11-09       Impact factor: 7.446

4.  Sexual Dimorphism in MAPK-Activated Protein Kinase-2 (MK2) Regulation of RANKL-Induced Osteoclastogenesis in Osteoclast Progenitor Subpopulations.

Authors:  Bethany A Herbert; Michael S Valerio; Matthias Gaestel; Keith L Kirkwood
Journal:  PLoS One       Date:  2015-05-06       Impact factor: 3.240

5.  Crystal structure of human cyclin-dependent kinase-2 complex with MK2 inhibitor TEI-I01800: insight into the selectivity.

Authors:  Aiko Fujino; Kei Fukushima; Takaharu Kubota; Tomomi Kosugi; Midori Takimoto-Kamimura
Journal:  J Synchrotron Radiat       Date:  2013-09-26       Impact factor: 2.616

6.  Comparative molecular dynamics simulations of mitogen-activated protein kinase-activated protein kinase 5.

Authors:  Inger Lindin; Yimingjiang Wuxiuer; Aina Westrheim Ravna; Ugo Moens; Ingebrigt Sylte
Journal:  Int J Mol Sci       Date:  2014-03-19       Impact factor: 5.923

Review 7.  MAPKAPK2: the master regulator of RNA-binding proteins modulates transcript stability and tumor progression.

Authors:  Sourabh Soni; Prince Anand; Yogendra S Padwad
Journal:  J Exp Clin Cancer Res       Date:  2019-03-08

8.  A computational study on thiourea analogs as potent MK-2 inhibitors.

Authors:  Ming Hao; Hong Ren; Fang Luo; Shuwei Zhang; Jieshan Qiu; Mingjuan Ji; Hongzong Si; Guohui Li
Journal:  Int J Mol Sci       Date:  2012-06-08       Impact factor: 6.208

  8 in total

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