Literature DB >> 19217782

Identification of a selective thieno[2,3-c]pyridine inhibitor of COT kinase and TNF-alpha production.

Kevin Cusack1, Hamish Allen, Agnieszka Bischoff, Anca Clabbers, Richard Dixon, Shannon Fix-Stenzel, Michael Friedman, Yvette Gaumont, Dawn George, Thomas Gordon, Pintipa Grongsaard, Bernd Janssen, Yong Jia, Maria Moskey, Christopher Quinn, Andres Salmeron, Christine Thomas, Grier Wallace, Neil Wishart, Zhengtian Yu.   

Abstract

COT (Tpl2 in mice) is a serine/threonine MAP3 kinase that regulates production of TNF-alpha and other pro-inflammatory cytokines such as IL-1beta via the ERK/MAP kinase pathway. As TNF-alpha and IL-1beta are clinically validated targets for therapeutic intervention in rheumatoid arthritis (RA), blocking COT provides a potential avenue for amelioration of disease. Herein we describe identification of a cellular active selective small molecule inhibitor of COT kinase.

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Year:  2009        PMID： 19217782     DOI： 10.1016/j.bmcl.2009.01.088

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


  8 in total

Review 1.  Macrophages in multiple myeloma: emerging concepts and therapeutic implications.

Authors:  Fotis Asimakopoulos; Jaehyup Kim; Ryan A Denu; Chelsea Hope; Jeffrey L Jensen; Samuel J Ollar; Ellen Hebron; Claire Flanagan; Natalie Callander; Peiman Hematti
Journal:  Leuk Lymphoma       Date:  2013-04-11

2.  Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.

Authors:  Michael F T Koehler; Philippe Bergeron; Elizabeth M Blackwood; Krista Bowman; Kevin R Clark; Ron Firestein; James R Kiefer; Klaus Maskos; Mark L McCleland; Linda Orren; Laurent Salphati; Steve Schmidt; Elisabeth V Schneider; Jiansheng Wu; Maureen H Beresini
Journal:  ACS Med Chem Lett       Date:  2016-01-06       Impact factor: 4.345

3.  Cot/tpl2 (MAP3K8) mediates myeloperoxidase activity and hypernociception following peripheral inflammation.

Authors:  Irene Soria-Castro; Agnieszka Krzyzanowska; Marta López Pelaéz; Javier Regadera; Gema Ferrer; Lluis Montoliu; Rosario Rodríguez-Ramos; Margarita Fernández; Susana Alemany
Journal:  J Biol Chem       Date:  2010-08-24       Impact factor: 5.157

4.  Tumor progression locus 2 (Tpl2) kinase promotes chemokine receptor expression and macrophage migration during acute inflammation.

Authors:  Sean M Rowley; Teneema Kuriakose; Lee M Dockery; Thi Tran-Nguyen; Aaron D Gingerich; Lai Wei; Wendy T Watford
Journal:  J Biol Chem       Date:  2014-04-08       Impact factor: 5.157

5.  Parsing out the complexity of RAF inhibitor resistance.

Authors:  Martin McMahon
Journal:  Pigment Cell Melanoma Res       Date:  2011-01-12       Impact factor: 4.693

6.  The Crystal Structure of Cancer Osaka Thyroid Kinase Reveals an Unexpected Kinase Domain Fold.

Authors:  Sascha Gutmann; Alexandra Hinniger; Gabriele Fendrich; Peter Drückes; Sylvie Antz; Henri Mattes; Henrik Möbitz; Silvio Ofner; Niko Schmiedeberg; Aleksandar Stojanovic; Sebastien Rieffel; André Strauss; Thomas Troxler; Ralf Glatthar; Helmut Sparrer
Journal:  J Biol Chem       Date:  2015-04-27       Impact factor: 5.157

Review 7.  Tumor progression locus 2 (Tpl2) kinase as a novel therapeutic target for cancer: double-sided effects of Tpl2 on cancer.

Authors:  Hye Won Lee; Han Yong Choi; Kyeung Min Joo; Do-Hyun Nam
Journal:  Int J Mol Sci       Date:  2015-02-25       Impact factor: 5.923

Review 8.  Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR cascade inhibitors: how mutations can result in therapy resistance and how to overcome resistance.

Authors:  James A McCubrey; Linda S Steelman; William H Chappell; Stephen L Abrams; Richard A Franklin; Giuseppe Montalto; Melchiorre Cervello; Massimo Libra; Saverio Candido; Grazia Malaponte; Maria C Mazzarino; Paolo Fagone; Ferdinando Nicoletti; Jörg Bäsecke; Sanja Mijatovic; Danijela Maksimovic-Ivanic; Michele Milella; Agostino Tafuri; Francesca Chiarini; Camilla Evangelisti; Lucio Cocco; Alberto M Martelli
Journal:  Oncotarget       Date:  2012-10
  8 in total

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