SB 203580 is a specific inhibitor of a MAP kinase homologue which is stimulated by cellular stresses and interleukin-1
Ana Cuenda,John Rouse,Yair N. Doza,Roger Meier,Philip Cohen,Timothy Francis Gallagher,Peter R. Young,John C. Lee +7 more
TLDR
It is established that MAPKAP kinase‐2 is a physiological RK substrate, and that HSP27 is phosphorylated by MAPK AP kinase-2 in vivo.About:
This article is published in FEBS Letters.The article was published on 1995-05-08 and is currently open access. It has received 2097 citations till now. The article focuses on the topics: SB 203580 & Mitogen-activated protein kinase kinase.read more
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Specificity and mechanism of action of some commonly used protein kinase inhibitors
TL;DR: The results demonstrate that the specificities of protein kinase inhibitors cannot be assessed simply by studying their effect on kinases that are closely related in primary structure, and proposes guidelines for the use of protein Kinase inhibitors in cell-based assays.
Journal ArticleDOI
PD 098059 Is a Specific Inhibitor of the Activation of Mitogen-activated Protein Kinase Kinase in Vitro and in Vivo
TL;DR: The results indicate that the activation of Raf is suppressed and that its inactivation is accelerated by a downstream component(s) of the MAP kinase pathway.
Journal ArticleDOI
Mechanism of activation of protein kinase B by insulin and IGF-1.
Dario R. Alessi,Mirjana Andjelkovic,Barry Caudwell,Peter Cron,Nick Morrice,Philip Cohen,Brian A. Hemmings +6 more
TL;DR: In this paper, the activation of PKBalpha was accompanied by its phosphorylation at Thr308 and Ser473 and, like activation, likeactivation was prevented by the phosphatidylinositol 3-kinase inhibitor wortmannin.
Journal ArticleDOI
The selectivity of protein kinase inhibitors: a further update.
Jenny Bain,Lorna Plater,Matthew Elliott,Natalia Shpiro,C. James Hastie,Hilary McLauchlan,Iva V. Klevernic,J. Simon C. Arthur,Dario R. Alessi,Philip Cohen +9 more
TL;DR: Harmine has been identified as a potent and specific inhibitor of DYRK1A (dual-specificity tyrosine-phosphorylated and -regulated kinase 1A) in vitro and the results have further emphasized the need for considerable caution in using small-molecule inhibitors of protein kinases to assess the physiological roles of these enzymes.
Journal ArticleDOI
A quantitative analysis of kinase inhibitor selectivity.
Mazen W. Karaman,Sanna Herrgard,Daniel K. Treiber,Paul Gallant,Corey E. Atteridge,Brian T. Campbell,Katrina W Chan,Pietro Ciceri,Mindy I. Davis,Philip T. Edeen,Raffaella Faraoni,Mark Floyd,Jeremy P. Hunt,Daniel J Lockhart,Zdravko V. Milanov,Michael J Morrison,Gabriel Pallares,Hitesh K. Patel,Stephanie Pritchard,Stephanie Pritchard,Lisa M. Wodicka,Patrick P. Zarrinkar +21 more
TL;DR: This work presents interaction maps for 38 kinase inhibitors across a panel of 317 kinases representing >50% of the predicted human protein kinome and introduces the concept of a selectivity score as a general tool to quantify and differentiate the observed interaction patterns.
References
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A protein kinase involved in the regulation of inflammatory cytokine biosynthesis.
Joseph C. Lee,Jeffrey T. Laydon,Peter C. McDonnell,Timothy Gallagher,Sanjay Kumar,David W. Green,Dean E. McNulty,M. J. Blumenthal,J. R. Heys,S. W. Landvatter,James E. Strickler,Megan M. McLaughlin,I. R. Siemens,Seth M. Fisher,George P. Livi,John R. White,Jerry L. Adams,Peter Young +17 more
TL;DR: Production of interleukin-1 and tumour necrosis factor from stimulated human monocytes is inhibited by a new series of pyridinyl-imidazole compounds, suggesting that the CSBPs are critical for cytokine production.
Journal ArticleDOI
JNK1: A protein kinase stimulated by UV light and Ha-Ras that binds and phosphorylates the c-Jun activation domain
Benoit Dérijard,Benoit Dérijard,Masahiko Hibi,I-Huan Wu,I-Huan Wu,Tamera Barrett,Bing Su,Tiliang Deng,Michael Karin,Roger J. Davis,Roger J. Davis +10 more
TL;DR: JNK1 is a component of a novel signal transduction pathway that is activated by oncoproteins and UV irradiation and its properties indicate that JNK1 activation may play an important role in tumor promotion.
Journal ArticleDOI
A MAP kinase targeted by endotoxin and hyperosmolarity in mammalian cells
TL;DR: Findings link a signaling pathway in mammalian cells with a pathway in yeast that is responsive to physiological stress.
Journal ArticleDOI
The stress-activated protein kinase subfamily of c-Jun kinases.
John M. Kyriakis,Papia Banerjee,Eleni Nikolakaki,Eleni Nikolakaki,Tianang Dai,Elizabeth A. Rubie,M. F. Ahmad,Joseph Avruch,James R. Woodgett +8 more
TL;DR: The kinase p54s are the principal c-Jun N-terminal kinases activated by cellular stress and tumour necrosis factor (TNF)-α, hence they are designated stress-activated protein kinases, or SAPKs.
Journal ArticleDOI
Identification of an oncoprotein- and UV-responsive protein kinase that binds and potentiates the c-Jun activation domain.
TL;DR: This work has identified a serine/threonine kinase whose activity is stimulated by the same signals that stimulate the amino-terminal phosphorylation of c-Jun, and suggests a mechanism through which protein kinase cascades can specifically modulate the activity of distinct nuclear targets.