2ghm: Difference between revisions
From Proteopedia
Jump to navigationJump to search
New page: left|200px<br /><applet load="2ghm" size="450" color="white" frame="true" align="right" spinBox="true" caption="2ghm, resolution 2.35Å" /> '''Mutated MAP kinase P... |
No edit summary |
||
| Line 1: | Line 1: | ||
[[Image:2ghm.gif|left|200px]]<br /><applet load="2ghm" size=" | [[Image:2ghm.gif|left|200px]]<br /><applet load="2ghm" size="350" color="white" frame="true" align="right" spinBox="true" | ||
caption="2ghm, resolution 2.35Å" /> | caption="2ghm, resolution 2.35Å" /> | ||
'''Mutated MAP kinase P38 (Mus Musculus) in complex with Inhbitor PG-895449'''<br /> | '''Mutated MAP kinase P38 (Mus Musculus) in complex with Inhbitor PG-895449'''<br /> | ||
==Overview== | ==Overview== | ||
A new class of tumor necrosis factor alpha (TNF-alpha) synthesis | A new class of tumor necrosis factor alpha (TNF-alpha) synthesis inhibitors based on an N-2,4-pyrimidine-N-phenyl-N'-phenyl urea scaffold is described. Many of these compounds showed low-nanomolar activity against lipopolysaccharide stimulated TNF-alpha production. X-ray co-crystallization studies with mutated p38alpha showed that these trisubstituted ureas interact with the ATP-binding pocket in a pseudo-bicyclic conformation brought about by the presence of an intramolecular hydrogen bonding interaction. | ||
==About this Structure== | ==About this Structure== | ||
2GHM 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 LIC as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] Full crystallographic information is available from [http:// | 2GHM 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=LIC:'>LIC</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GHM OCA]. | ||
==Reference== | ==Reference== | ||
| Line 14: | Line 14: | ||
[[Category: Non-specific serine/threonine protein kinase]] | [[Category: Non-specific serine/threonine protein kinase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Evdokimov, A | [[Category: Evdokimov, A G.]] | ||
[[Category: Maier, J | [[Category: Maier, J A.]] | ||
[[Category: Mekel, M | [[Category: Mekel, M J.]] | ||
[[Category: Pokross, M | [[Category: Pokross, M E.]] | ||
[[Category: Walter, R | [[Category: Walter, R L.]] | ||
[[Category: LIC]] | [[Category: LIC]] | ||
[[Category: map kinase p38]] | [[Category: map kinase p38]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:31:46 2008'' | ||
