2gtm: Difference between revisions
New page: left|200px<br /><applet load="2gtm" size="450" color="white" frame="true" align="right" spinBox="true" caption="2gtm, resolution 1.90Å" /> '''Mutated Mouse P38 MA... |
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[[Image:2gtm.gif|left|200px]]<br /><applet load="2gtm" size=" | [[Image:2gtm.gif|left|200px]]<br /><applet load="2gtm" size="350" color="white" frame="true" align="right" spinBox="true" | ||
caption="2gtm, resolution 1.90Å" /> | caption="2gtm, resolution 1.90Å" /> | ||
'''Mutated Mouse P38 MAP Kinase Domain in complex with Inhibitor PG-892579'''<br /> | '''Mutated Mouse P38 MAP Kinase Domain in complex with Inhibitor PG-892579'''<br /> | ||
==Overview== | ==Overview== | ||
A series of C-2, C-8, and N-9 trisubstituted purine based inhibitors of | 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). | ||
==About this Structure== | ==About this Structure== | ||
2GTM is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus] with LID as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Mitogen-activated_protein_kinase Mitogen-activated protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.24 2.7.11.24] Full crystallographic information is available from [http:// | 2GTM is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus] with <scene name='pdbligand=LID:'>LID</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Mitogen-activated_protein_kinase Mitogen-activated protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.24 2.7.11.24] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GTM OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Mus musculus]] | [[Category: Mus musculus]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Evdokimov, A | [[Category: Evdokimov, A G.]] | ||
[[Category: Mekel, M | [[Category: Mekel, M J.]] | ||
[[Category: Pokross, M | [[Category: Pokross, M E.]] | ||
[[Category: Sabat, M.]] | [[Category: Sabat, M.]] | ||
[[Category: Walter, R | [[Category: Walter, R L.]] | ||
[[Category: LID]] | [[Category: LID]] | ||
[[Category: map kinase p38]] | [[Category: map kinase p38]] | ||
[[Category: p38]] | [[Category: p38]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:35:15 2008'' | ||
