View source for 2ghl

[[Image:2ghl.gif|left|200px]]

 {{Structure
|PDB= 2ghl |SIZE=350|CAPTION= <scene name='initialview01'>2ghl</scene>, resolution 2.099&Aring;
|SITE= 
|LIGAND= <scene name='pdbligand=LIB:3-(2-CHLOROPHENYL)-1-(2-{[(1S)-2-HYDROXY-1,2-DIMETHYLPROPYL]AMINO}PYRIMIDIN-4-YL)-1-(4-METHOXYPHENYL)UREA'>LIB</scene>
|ACTIVITY= [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] 
|GENE= Mapk14, Crk1, Csbp1, Csbp2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 Mus musculus])
}}

'''Mutant Mus Musculus P38 Kinase Domain in Complex with Inhibitor PG-874743'''


==Overview==
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==
2GHL is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GHL OCA]. 

==Reference==
Development of N-2,4-pyrimidine-N-phenyl-N'-phenyl ureas as inhibitors of tumor necrosis factor alpha (TNF-alpha) synthesis. Part 1., Brugel TA, Maier JA, Clark MP, Sabat M, Golebiowski A, Bookland RG, Laufersweiler MJ, Laughlin SK, Vanrens JC, De B, Hsieh LC, Mekel MJ, Janusz MJ, Bioorg Med Chem Lett. 2006 Jul 1;16(13):3510-3. Epub 2006 May 2. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16632356 16632356]
[[Category: Mus musculus]]
[[Category: Non-specific serine/threonine protein kinase]]
[[Category: Single protein]]
[[Category: Brugel, T A.]]
[[Category: Evdokimov, A G.]]
[[Category: Mekel, M J.]]
[[Category: Pokross, M E.]]
[[Category: Walter, R L.]]
[[Category: LIB]]
[[Category: map kinase p38]]
[[Category: p38]]

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