3c5u

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{{STRUCTURE_3c5u| PDB=3c5u | SCENE= }}
{{STRUCTURE_3c5u| PDB=3c5u | SCENE= }}
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'''P38 ALPHA map kinase complexed with a benzothiazole based inhibitor'''
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===P38 ALPHA map kinase complexed with a benzothiazole based inhibitor===
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==Overview==
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Rational design, synthesis, and SAR studies of a novel class of benzothiazole based inhibitors of p38alpha MAP kinase are described. The issue of metabolic instability associated with vicinal phenyl, benzo[d]thiazol-6-yl oxazoles/imidazoles was addressed by the replacement of the central oxazole or imidazole ring with an aminopyrazole system. The proposed binding mode of this new class of p38alpha inhibitors was confirmed by X-ray crystallographic studies of a representative inhibitor (6a) bound to the p38alpha enzyme.
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{{ABSTRACT_PUBMED_18296051}}
==About this Structure==
==About this Structure==
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[[Category: Serine/threonine-protein kinase]]
[[Category: Serine/threonine-protein kinase]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed May 7 08:59:55 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 15:56:37 2008''

Revision as of 12:56, 29 July 2008

Image:3c5u.png

Template:STRUCTURE 3c5u

P38 ALPHA map kinase complexed with a benzothiazole based inhibitor

Template:ABSTRACT PUBMED 18296051

About this Structure

3C5U is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Benzothiazole based inhibitors of p38alpha MAP kinase., Liu C, Lin J, Pitt S, Zhang RF, Sack JS, Kiefer SE, Kish K, Doweyko AM, Zhang H, Marathe PH, Trzaskos J, Mckinnon M, Dodd JH, Barrish JC, Schieven GL, Leftheris K, Bioorg Med Chem Lett. 2008 Mar 15;18(6):1874-9. Epub 2008 Feb 10. PMID:18296051

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