2gtm

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[[Image:2gtm.gif|left|200px]]
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{{STRUCTURE_2gtm| PDB=2gtm | SCENE= }}
{{STRUCTURE_2gtm| PDB=2gtm | SCENE= }}
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'''Mutated Mouse P38 MAP Kinase Domain in complex with Inhibitor PG-892579'''
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===Mutated Mouse P38 MAP Kinase Domain in complex with Inhibitor PG-892579===
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==Overview==
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A series of C-2, C-8, and N-9 trisubstituted purine based inhibitors of TNF-alpha production are described. The most potent analogs showed low nanomolar activity against LPS-induced TNF-alpha production in a THP-1 cell based assay. The SAR of the series was optimized with the aid of X-ray co-crystal structures of these inhibitors bound with mutated p38 (mp38).
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(as it appears on PubMed at http://www.pubmed.gov), where 16750367 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16750367}}
==About this Structure==
==About this Structure==
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[[Category: Map kinase p38]]
[[Category: Map kinase p38]]
[[Category: P38]]
[[Category: P38]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:31:15 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 19:24:05 2008''

Revision as of 16:24, 27 July 2008

Template:STRUCTURE 2gtm

Mutated Mouse P38 MAP Kinase Domain in complex with Inhibitor PG-892579

Template:ABSTRACT PUBMED 16750367

About this Structure

2GTM is a Single protein structure of sequence from Mus musculus. Full crystallographic information is available from OCA.

Reference

The development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-alpha production., Sabat M, Vanrens JC, Clark MP, Brugel TA, Maier J, Bookland RG, Laufersweiler MJ, Laughlin SK, Golebiowski A, De B, Hsieh LC, Walter RL, Mekel MJ, Janusz MJ, Bioorg Med Chem Lett. 2006 Aug 15;16(16):4360-5. Epub 2006 Jun 5. PMID:16750367

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