Literature DB >> 22198732

Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor.

Solveigh C Koeberle1, Johannes Romir, Stefan Fischer, Andreas Koeberle, Verena Schattel, Wolfgang Albrecht, Christian Grütter, Oliver Werz, Daniel Rauh, Thilo Stehle, Stefan A Laufer.   

Abstract

Until now, a lack of inhibitors with high potency and selectivity in vivo has hampered investigation of the p38 mitogen-activated protein kinase (MAPK) signaling pathway. We describe the design of skepinone-L, which is, to our knowledge, the first ATP-competitive p38 MAPK inhibitor with excellent in vivo efficacy and selectivity. Therefore, skepinone-L is a valuable probe for chemical biology research, and it may foster the development of a unique class of kinase inhibitors.

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Year:  2011        PMID： 22198732     DOI： 10.1038/nchembio.761

Source DB:  PubMed          Journal:  Nat Chem Biol        ISSN： 1552-4450            Impact factor:   15.040


  24 in total

Review 1.  The protein kinase complement of the human genome.

Authors:  G Manning; D B Whyte; R Martinez; T Hunter; S Sudarsanam
Journal:  Science       Date:  2002-12-06       Impact factor: 47.728

Review 2.  MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alpha protein.

Authors:  Matthew R Lee; Celia Dominguez
Journal:  Curr Med Chem       Date:  2005       Impact factor: 4.530

Review 3.  The p38 mitogen-activated protein kinase (MAPK) pathway in rheumatoid arthritis.

Authors:  G Schett; J Zwerina; G Firestein
Journal:  Ann Rheum Dis       Date:  2007-09-07       Impact factor: 19.103

4.  A quantitative analysis of kinase inhibitor selectivity.

Authors:  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; Lisa M Wodicka; Patrick P Zarrinkar
Journal:  Nat Biotechnol       Date:  2008-01       Impact factor: 54.908

5.  Activation of p38 and ERK signaling during adenovirus vector cell entry lead to expression of the C-X-C chemokine IP-10.

Authors:  Lee Anne Tibbles; Jason C L Spurrell; Gloria P Bowen; Qiang Liu; Mindy Lam; Anne K Zaiss; Stephen M Robbins; Morley D Hollenberg; Thomas J Wickham; Daniel A Muruve
Journal:  J Virol       Date:  2002-02       Impact factor: 5.103

6.  Design, synthesis, and biological evaluation of phenylamino-substituted 6,11-dihydro-dibenzo[b,e]oxepin-11-ones and dibenzo[a,d]cycloheptan-5-ones: novel p38 MAP kinase inhibitors.

Authors:  Stefan A Laufer; Gabriele M Ahrens; Solveigh C Karcher; Jörg S Hering; Raimund Niess
Journal:  J Med Chem       Date:  2006-12-28       Impact factor: 7.446

7.  Rho kinase-2 activation in human endothelial cells drives lysophosphatidic acid-mediated expression of cell adhesion molecules via NF-kappaB p65.

Authors:  Hideaki Shimada; Lakshman E Rajagopalan
Journal:  J Biol Chem       Date:  2010-02-17       Impact factor: 5.157

8.  The p38 mitogen-activated protein kinase pathway plays a critical role in PAR2-induced endothelial IL-8 production and leukocyte adhesion.

Authors:  Shiow L Pan; Kai Y Tao; Jih H Guh; Hui L Sun; Der Y Huang; Ya L Chang; Che M Teng
Journal:  Shock       Date:  2008-11       Impact factor: 3.454

Review 9.  Successful structure-based design of recent p38 MAP kinase inhibitors.

Authors:  Solveigh C Karcher; Stefan A Laufer
Journal:  Curr Top Med Chem       Date:  2009       Impact factor: 3.295

10.  Pamapimod, a novel p38 mitogen-activated protein kinase inhibitor: preclinical analysis of efficacy and selectivity.

Authors:  Ronald J Hill; Karim Dabbagh; Deborah Phippard; Ching Li; Rebecca T Suttmann; Mary Welch; Eva Papp; Kyung W Song; Kung-Ching Chang; David Leaffer; Yong-Nam Kim; Richard T Roberts; Tanja S Zabka; Dee Aud; Joseph Dal Porto; Anthony M Manning; Stanford L Peng; David M Goldstein; Brian R Wong
Journal:  J Pharmacol Exp Ther       Date:  2008-09-05       Impact factor: 4.030
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  37 in total

1.  Spinal inhibition of p38 MAP kinase reduces inflammatory and neuropathic pain in male but not female mice: Sex-dependent microglial signaling in the spinal cord.

Authors:  Sarah Taves; Temugin Berta; Da-Lu Liu; Sophie Gan; Gang Chen; Yong Ho Kim; Thomas Van de Ven; Stefan Laufer; Ru-Rong Ji
Journal:  Brain Behav Immun       Date:  2015-10-19       Impact factor: 7.217

2.  The ins and outs of selective kinase inhibitor development.

Authors:  Susanne Müller; Apirat Chaikuad; Nathanael S Gray; Stefan Knapp
Journal:  Nat Chem Biol       Date:  2015-11       Impact factor: 15.040

3.  A Chemical Probe Strategy for Interrogating Inhibitor Selectivity Across the MEK Kinase Family.

Authors:  Kristine K Deibler; Rama K Mishra; Matthew R Clutter; Aleksandar Antanasijevic; Raymond Bergan; Michael Caffrey; Karl A Scheidt
Journal:  ACS Chem Biol       Date:  2017-03-20       Impact factor: 5.100

4.  Temperoammonic Stimulation Depotentiates Schaffer Collateral LTP via p38 MAPK Downstream of Adenosine A1 Receptors.

Authors:  Yukitoshi Izumi; Charles F Zorumski
Journal:  J Neurosci       Date:  2019-01-08       Impact factor: 6.167

5.  The crystal structure of phosphorylated MAPK13 reveals common structural features and differences in p38 MAPK family activation.

Authors:  Zeynep Yurtsever; Suzanne M Scheaffer; Arthur G Romero; Michael J Holtzman; Tom J Brett
Journal:  Acta Crystallogr D Biol Crystallogr       Date:  2015-03-26

6.  Intrathecal administration of antisense oligonucleotide against p38α but not p38β MAP kinase isoform reduces neuropathic and postoperative pain and TLR4-induced pain in male mice.

Authors:  Xin Luo; Bethany Fitzsimmons; Apoorva Mohan; Linlin Zhang; Niccolo Terrando; Holly Kordasiewicz; Ru-Rong Ji
Journal:  Brain Behav Immun       Date:  2017-11-08       Impact factor: 7.217

7.  Elucidation of cGMP-dependent induction of mitochondrial biogenesis through PKG and p38 MAPK in the kidney.

Authors:  Pallavi Bhargava; Jaroslav Janda; Rick G Schnellmann
Journal:  Am J Physiol Renal Physiol       Date:  2019-12-16

8.  Evaluation of the therapeutic potential of the selective p38 MAPK inhibitor Skepinone-L and the dual p38/JNK 3 inhibitor LN 950 in experimental K/BxN serum transfer arthritis.

Authors:  Philipp Guenthoer; Kerstin Fuchs; Gerald Reischl; Leticia Quintanilla-Martinez; Irene Gonzalez-Menendez; Stefan Laufer; Bernd J Pichler; Manfred Kneilling
Journal:  Inflammopharmacology       Date:  2019-04-29       Impact factor: 4.473

9.  Arachidonoyl-phosphatidylcholine oscillates during the cell cycle and counteracts proliferation by suppressing Akt membrane binding.

Authors:  Andreas Koeberle; Hideo Shindou; Solveigh C Koeberle; Stefan A Laufer; Takao Shimizu; Oliver Werz
Journal:  Proc Natl Acad Sci U S A       Date:  2013-01-28       Impact factor: 11.205

10.  First comprehensive structural and biophysical analysis of MAPK13 inhibitors targeting DFG-in and DFG-out binding modes.

Authors:  Zeynep Yurtsever; Dhara A Patel; Daniel L Kober; Alvin Su; Chantel A Miller; Arthur G Romero; Michael J Holtzman; Tom J Brett
Journal:  Biochim Biophys Acta       Date:  2016-06-29
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