1ywr

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{{STRUCTURE_1ywr| PDB=1ywr | SCENE= }}
{{STRUCTURE_1ywr| PDB=1ywr | SCENE= }}
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'''Crystal Structure Analysis of inactive P38 kinase domain in complex with a Monocyclic Pyrazolone Inhibitor'''
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===Crystal Structure Analysis of inactive P38 kinase domain in complex with a Monocyclic Pyrazolone Inhibitor===
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==Overview==
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4-Aryl-5-pyrimidyl based cytokine synthesis inhibitors that contain a novel monocyclic, pyrazolone heterocyclic core are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-alpha production. One of the compounds (6e) was found to be efficacious in the rat iodoacetate (RIA) in vivo model of osteoarthritis. The X-ray crystal structure of a pyrazolone inhibitor cocrystallized with mutated p38 (mp38) is presented.
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The line below this paragraph, {{ABSTRACT_PUBMED_15837310}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 15837310 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15837310}}
==About this Structure==
==About this Structure==
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[[Category: Moncyclic pyrazolone]]
[[Category: Moncyclic pyrazolone]]
[[Category: P38 kinase]]
[[Category: P38 kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 16:53:45 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 19:55:57 2008''

Revision as of 16:56, 28 July 2008

Image:1ywr.png

Template:STRUCTURE 1ywr

Crystal Structure Analysis of inactive P38 kinase domain in complex with a Monocyclic Pyrazolone Inhibitor

Template:ABSTRACT PUBMED 15837310

About this Structure

1YWR is a Single protein structure of sequence from Mus musculus. Full crystallographic information is available from OCA.

Reference

The development of monocyclic pyrazolone based cytokine synthesis inhibitors., Golebiowski A, Townes JA, Laufersweiler MJ, Brugel TA, Clark MP, Clark CM, Djung JF, Laughlin SK, Sabat MP, Bookland RG, VanRens JC, De B, Hsieh LC, Janusz MJ, Walter RL, Webster ME, Mekel MJ, Bioorg Med Chem Lett. 2005 May 2;15(9):2285-9. PMID:15837310

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