Literature DB >> 12617920

Discovery of novel and selective IKK-beta serine-threonine protein kinase inhibitors. Part 1.

Toshiki Murata1, Mitsuyuki Shimada, Sachiko Sakakibara, Takashi Yoshino, Hiroshi Kadono, Tsutomu Masuda, Makoto Shimazaki, Takuya Shintani, Kinji Fuchikami, Katsuya Sakai, Hisayo Inbe, Keisuke Takeshita, Toshiro Niki, Masaomi Umeda, Kevin B Bacon, Karl B Ziegelbauer, Timothy B Lowinger.   

Abstract

IkappaB kinase beta (IKK-beta) is a serine-threonine protein kinase critically involved in the activation of the transcription factor Nuclear Factor kappa B (NF-kappaB) in response to various inflammatory stimuli. We have identified a small molecule inhibitor of IKK-beta. Optimization of the lead compound resulted in improvements in both in vitro and in vivo potency, and provided IKK-beta inhibitors exhibiting potent activity in an acute cytokine release model (LPS-induced TNFalpha).

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Year:  2003        PMID： 12617920     DOI： 10.1016/s0960-894x(02)01046-6

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


  26 in total

1.  Inhibition of human immunodeficiency virus type 1 replication in latently infected cells by a novel IkappaB kinase inhibitor.

Authors:  Ann Florence B Victoriano; Kaori Asamitsu; Yurina Hibi; Kenichi Imai; Nina G Barzaga; Takashi Okamoto
Journal:  Antimicrob Agents Chemother       Date:  2006-02       Impact factor: 5.191

2.  Beyond the frog: the evolution of homology models of human IKKβ.

Authors:  Nicholas Y Palermo; Amarnath Natarajan
Journal:  Bioorg Med Chem Lett       Date:  2011-08-19       Impact factor: 2.823

Review 3.  Inhibitory kappa B Kinases as targets for pharmacological regulation.

Authors:  Carly Gamble; Kathryn McIntosh; Rebecca Scott; Ka Ho Ho; Robin Plevin; Andrew Paul
Journal:  Br J Pharmacol       Date:  2012-02       Impact factor: 8.739

4.  Targeting the Canonical Nuclear Factor-κB Pathway with a High-Potency IKK2 Inhibitor Improves Outcomes in a Mouse Model of Idiopathic Pneumonia Syndrome.

Authors:  Kenneth A Fowler; Corey M Jania; Stephen L Tilley; Angela Panoskaltsis-Mortari; Albert S Baldwin; Jonathan S Serody; James M Coghill
Journal:  Biol Blood Marrow Transplant       Date:  2017-02-01       Impact factor: 5.742

5.  A selective novel low-molecular-weight inhibitor of IkappaB kinase-beta (IKK-beta) prevents pulmonary inflammation and shows broad anti-inflammatory activity.

Authors:  Karl Ziegelbauer; Florian Gantner; Nicholas W Lukacs; Aaron Berlin; Kinji Fuchikami; Toshiro Niki; Katsuya Sakai; Hisayo Inbe; Keisuke Takeshita; Mina Ishimori; Hiroshi Komura; Toshiki Murata; Timothy Lowinger; Kevin B Bacon
Journal:  Br J Pharmacol       Date:  2005-05       Impact factor: 8.739

6.  IκB kinase β (IKKβ) inhibits p63 isoform γ (TAp63γ) transcriptional activity.

Authors:  Jun-Ming Liao; Yu Zhang; Wenjuan Liao; Sheyla X Zeng; Xiaohua Su; Elsa R Flores; Hua Lu
Journal:  J Biol Chem       Date:  2013-04-15       Impact factor: 5.157

7.  Discovery of a novel IKK-β inhibitor by ligand-based virtual screening techniques.

Authors:  Stefan M Noha; Atanas G Atanasov; Daniela Schuster; Patrick Markt; Nanang Fakhrudin; Elke H Heiss; Olivia Schrammel; Judith M Rollinger; Hermann Stuppner; Verena M Dirsch; Gerhard Wolber
Journal:  Bioorg Med Chem Lett       Date:  2010-10-20       Impact factor: 2.823

8.  Identification of human IKK-2 inhibitors of natural origin (part I): modeling of the IKK-2 kinase domain, virtual screening and activity assays.

Authors:  Esther Sala; Laura Guasch; Justyna Iwaszkiewicz; Miquel Mulero; Maria-Josepa Salvadó; Montserrat Pinent; Vincent Zoete; Aurélien Grosdidier; Santiago Garcia-Vallvé; Olivier Michielin; Gerard Pujadas
Journal:  PLoS One       Date:  2011-02-24       Impact factor: 3.240

9.  2-Amino-6-(dimethyl-amino)pyridine-3,5-dicarbonitrile.

Authors:  Shaaban K Mohamed; Ahmed M Soliman; Eman M M Abdel-Raheem; Sohail Saeed; Wing-Tak Wong
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-04-25

Review 10.  Gene therapy targeting nuclear factor-kappaB: towards clinical application in inflammatory diseases and cancer.

Authors:  Sander W Tas; Margriet J B M Vervoordeldonk; Paul P Tak
Journal:  Curr Gene Ther       Date:  2009-06       Impact factor: 4.391
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