2gtm: Difference between revisions

Revision as of 05:31, 4 May 2008

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

OverviewOverview

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 StructureAbout this Structure

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

ReferenceReference

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 Page seeded by OCA on Sun May 4 05:31:15 2008

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA

@@ Line 1: / Line 1: @@
 [[Image:2gtm.gif|left|200px]]
- {{Structure
+<!--
-|PDB= 2gtm |SIZE=350|CAPTION= <scene name='initialview01'>2gtm</scene>, resolution 1.90&Aring;
+The line below this paragraph, containing "STRUCTURE_2gtm", creates the "Structure Box" on the page.
-|SITE=
+You may change the PDB parameter (which sets the PDB file loaded into the applet)
-|LIGAND= <scene name='pdbligand=LID:8-(2-CHLOROPHENYLAMINO)-2-(2,6-DIFLUOROPHENYLAMINO)-9-ETHYL-9H-PURINE-1,7-DIIUM'>LID</scene>
+or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-|ACTIVITY= <span class='plainlinks'>[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] </span>
+or leave the SCENE parameter empty for the default display.
-|GENE= Mapk14 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 Mus musculus])
+-->
-|DOMAIN=
+{{STRUCTURE_2gtm|  PDB=2gtm  |  SCENE=  }}
-|RELATEDENTRY=[[1yw2|1YW2]], [[1ywr|1YWR]], [[2ghm|2GHM]], [[2ghl|2GHL]]
-|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2gtm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2gtm OCA], [http://www.ebi.ac.uk/pdbsum/2gtm PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2gtm RCSB]</span>
-}}
 '''Mutated Mouse P38 MAP Kinase Domain in complex with Inhibitor PG-892579'''
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 [[Category: Sabat, M.]]
 [[Category: Walter, R L.]]
-[[Category: map kinase p38]]
+[[Category: Map kinase p38]]
-[[Category: p38]]
+[[Category: P38]]
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 05:31:15 2008''
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:21:24 2008''