1yqj

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[[Image:1yqj.gif|left|200px]]
[[Image:1yqj.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1yqj |SIZE=350|CAPTION= <scene name='initialview01'>1yqj</scene>, resolution 2.00&Aring;
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The line below this paragraph, containing "STRUCTURE_1yqj", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=6NP:6((S)-3-BENZYLPIPERAZIN-1-YL)-3-(NAPHTHALEN-2-YL)-4-(PYRIDIN-4-YL)PYRAZINE'>6NP</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[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] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= MAPK14, CSBP, CSBP1, CSBP2, MXI2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_1yqj| PDB=1yqj | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1yqj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yqj OCA], [http://www.ebi.ac.uk/pdbsum/1yqj PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1yqj RCSB]</span>
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}}
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'''Crystal Structure of p38 Alpha in Complex with a Selective Pyridazine Inhibitor'''
'''Crystal Structure of p38 Alpha in Complex with a Selective Pyridazine Inhibitor'''
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[[Category: Wong, M L.]]
[[Category: Wong, M L.]]
[[Category: Yu, V.]]
[[Category: Yu, V.]]
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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 16:39:15 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:18:22 2008''
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Revision as of 13:39, 3 May 2008

Image:1yqj.gif

Template:STRUCTURE 1yqj

Crystal Structure of p38 Alpha in Complex with a Selective Pyridazine Inhibitor


Overview

Novel potent trisubstituted pyridazine inhibitors of p38 MAP (mitogen activated protein) kinase are described that have activity in both cell-based assays of cytokine release and animal models of rheumatoid arthritis. They demonstrated potent inhibition of LPS-induced TNF-alpha production in mice and exhibited good efficacy in the rat collagen induced arthritis model.

About this Structure

1YQJ is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase., Tamayo N, Liao L, Goldberg M, Powers D, Tudor YY, Yu V, Wong LM, Henkle B, Middleton S, Syed R, Harvey T, Jang G, Hungate R, Dominguez C, Bioorg Med Chem Lett. 2005 May 2;15(9):2409-13. PMID:15837335 Page seeded by OCA on Sat May 3 16:39:15 2008

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OCA

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