1yqj

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[[Image:1yqj.gif|left|200px]]<br /><applet load="1yqj" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1yqj.gif|left|200px]]
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caption="1yqj, resolution 2.00&Aring;" />
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'''Crystal Structure of p38 Alpha in Complex with a Selective Pyridazine Inhibitor'''<br />
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{{Structure
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|PDB= 1yqj |SIZE=350|CAPTION= <scene name='initialview01'>1yqj</scene>, resolution 2.00&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene> and <scene name='pdbligand=6NP:6((S)-3-BENZYLPIPERAZIN-1-YL)-3-(NAPHTHALEN-2-YL)-4-(PYRIDIN-4-YL)PYRAZINE'>6NP</scene>
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|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]
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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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'''Crystal Structure of p38 Alpha in Complex with a Selective Pyridazine Inhibitor'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1YQJ is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SO4:'>SO4</scene> and <scene name='pdbligand=6NP:'>6NP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. 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=1YQJ OCA].
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1YQJ is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1YQJ OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15837335 15837335]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/15837335 15837335]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Non-specific serine/threonine protein kinase]]
[[Category: Non-specific serine/threonine protein kinase]]
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[[Category: transferase]]
[[Category: transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:08:05 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 15:26:11 2008''

Revision as of 13:26, 20 March 2008

Image:1yqj.gif


PDB ID 1yqj

Drag the structure with the mouse to rotate
, resolution 2.00Å
Ligands: and
Gene: MAPK14, CSBP, CSBP1, CSBP2, MXI2 (Homo sapiens)
Activity: Non-specific serine/threonine protein kinase, with EC number 2.7.11.1
Coordinates: save as pdb, mmCIF, xml



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 Thu Mar 20 15:26:11 2008

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