Literature DB >> 20045647

Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.

Surya K De1, Vida Chen, John L Stebbins, Li-Hsing Chen, Jason F Cellitti, Thomas Machleidt, Elisa Barile, Megan Riel-Mehan, Russell Dahl, Li Yang, Aras Emdadi, Ria Murphy, Maurizio Pellecchia.   

Abstract

A series of thiadiazole derivatives has been designed as potential allosteric, substrate competitive inhibitors of the protein kinase JNK. We report on the synthesis, characterization and evaluation of a series of compounds that resulted in the identification of potent and selective JNK inhibitors targeting its JIP-1 docking site. Copyright 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID： 20045647      PMCID： PMC2818674          DOI： 10.1016/j.bmc.2009.12.013

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  27 in total

1.  Selective interaction of JNK protein kinase isoforms with transcription factors.

Authors:  S Gupta; T Barrett; A J Whitmarsh; J Cavanagh; H K Sluss; B Dérijard; R J Davis
Journal:  EMBO J       Date:  1996-06-03       Impact factor: 11.598

2.  Design, synthesis, and biological activity of novel, potent, and selective (benzoylaminomethyl)thiophene sulfonamide inhibitors of c-Jun-N-terminal kinase.

Authors:  Thomas Rückle; Marco Biamonte; Tania Grippi-Vallotton; Steve Arkinstall; Yves Cambet; Montserrat Camps; Christian Chabert; Dennis J Church; Serge Halazy; Xuliang Jiang; Isabelle Martinou; Anthony Nichols; Wolfgang Sauer; Jean-Pierre Gotteland
Journal:  J Med Chem       Date:  2004-12-30       Impact factor: 7.446

3.  Development of paramagnetic probes for molecular recognition studies in protein kinases.

Authors:  Jesus Vazquez; Surya K De; Li-Hsing Chen; Megan Riel-Mehan; Aras Emdadi; Jason Cellitti; John L Stebbins; Michele F Rega; Maurizio Pellecchia
Journal:  J Med Chem       Date:  2008-06-26       Impact factor: 7.446

4.  Differential targeting of MAP kinases to the ETS-domain transcription factor Elk-1.

Authors:  S H Yang; A J Whitmarsh; R J Davis; A D Sharrocks
Journal:  EMBO J       Date:  1998-03-16       Impact factor: 11.598

5.  Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase.

Authors:  Pascale Gaillard; Isabelle Jeanclaude-Etter; Vittoria Ardissone; Steve Arkinstall; Yves Cambet; Montserrat Camps; Christian Chabert; Dennis Church; Rocco Cirillo; Denise Gretener; Serge Halazy; Anthony Nichols; Cedric Szyndralewiez; Pierre-Alain Vitte; Jean-Pierre Gotteland
Journal:  J Med Chem       Date:  2005-07-14       Impact factor: 7.446

6.  Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors.

Authors:  Hongyu Zhao; Michael D Serby; Zhili Xin; Bruce G Szczepankiewicz; Mei Liu; Christi Kosogof; Bo Liu; Lissa T J Nelson; Eric F Johnson; Sanyi Wang; Terry Pederson; Rebecca J Gum; Jill E Clampit; Deanna L Haasch; Cele Abad-Zapatero; Elizabeth H Fry; Cristina Rondinone; James M Trevillyan; Hing L Sham; Gang Liu
Journal:  J Med Chem       Date:  2006-07-27       Impact factor: 7.446

7.  Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-Jun N-terminal kinase.

Authors:  Surya K De; John L Stebbins; Li-Hsing Chen; Megan Riel-Mehan; Thomas Machleidt; Russell Dahl; Hongbin Yuan; Aras Emdadi; Elisa Barile; Vida Chen; Ria Murphy; Maurizio Pellecchia
Journal:  J Med Chem       Date:  2009-04-09       Impact factor: 7.446

8.  Identification of a new JNK inhibitor targeting the JNK-JIP interaction site.

Authors:  John L Stebbins; Surya K De; Thomas Machleidt; Barbara Becattini; Jesus Vazquez; Christian Kuntzen; Li-Hsing Chen; Jason F Cellitti; Megan Riel-Mehan; Aras Emdadi; Giovanni Solinas; Michael Karin; Maurizio Pellecchia
Journal:  Proc Natl Acad Sci U S A       Date:  2008-10-15       Impact factor: 11.205

9.  Identification of small-molecule inhibitors of the JIP-JNK interaction.

Authors:  Tracy Chen; Natasha Kablaoui; Jeremy Little; Sergei Timofeevski; William R Tschantz; Ping Chen; Junli Feng; Maura Charlton; Robert Stanton; Paul Bauer
Journal:  Biochem J       Date:  2009-05-13       Impact factor: 3.857

Review 10.  Inhibitors of c-Jun N-terminal kinases: JuNK no more?

Authors:  Marie A Bogoyevitch; Peter G Arthur
Journal:  Biochim Biophys Acta       Date:  2007-10-11
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  5 in total

Review 1.  Computational insights for the discovery of non-ATP competitive inhibitors of MAP kinases.

Authors:  Michael J Schnieders; Tamer S Kaoud; Chunli Yan; Kevin N Dalby; Pengyu Ren
Journal:  Curr Pharm Des       Date:  2012       Impact factor: 3.116

2.  Design and characterization of a potent and selective dual ATP- and substrate-competitive subnanomolar bidentate c-Jun N-terminal kinase (JNK) inhibitor.

Authors:  John L Stebbins; Surya K De; Petra Pavlickova; Vida Chen; Thomas Machleidt; Li-Hsing Chen; Christian Kuntzen; Shinichi Kitada; Michael Karin; Maurizio Pellecchia
Journal:  J Med Chem       Date:  2011-08-23       Impact factor: 7.446

3.  Inhibition of JNK mitochondrial localization and signaling is protective against ischemia/reperfusion injury in rats.

Authors:  Jeremy W Chambers; Alok Pachori; Shannon Howard; Sarah Iqbal; Philip V LoGrasso
Journal:  J Biol Chem       Date:  2012-12-20       Impact factor: 5.157

4.  A fluorescence-based assay for p38α recruitment site binders: identification of rooperol as a novel p38α kinase inhibitor.

Authors:  Jing Li; Tamer S Kaoud; Jake LeVieux; Brad Gilbreath; Swapna Moharana; Kevin N Dalby; Sean M Kerwin
Journal:  Chembiochem       Date:  2012-12-06       Impact factor: 3.164

5.  From in Silico Discovery to intra-Cellular Activity: Targeting JNK-Protein Interactions with Small Molecules.

Authors:  Tamer S Kaoud; Chunli Yan; Shreya Mitra; Chun-Chia Tseng; Jiney Jose; Juliana M Taliaferro; Maidina Tuohetahuntila; Ashwini Devkota; Rachel Sammons; Jihyun Park; Heekwang Park; Yue Shi; Jiyong Hong; Pengyu Ren; Kevin N Dalby
Journal:  ACS Med Chem Lett       Date:  2012-08-06       Impact factor: 4.345
  5 in total

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