1yqj
From Proteopedia
(New page: 200px<br /> <applet load="1yqj" size="450" color="white" frame="true" align="right" spinBox="true" caption="1yqj, resolution 2.00Å" /> '''Crystal Structure o...) |
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| - | [[Image:1yqj.gif|left|200px]]<br /> | + | [[Image:1yqj.gif|left|200px]]<br /><applet load="1yqj" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="1yqj, resolution 2.00Å" /> | caption="1yqj, resolution 2.00Å" /> | ||
'''Crystal Structure of p38 Alpha in Complex with a Selective Pyridazine Inhibitor'''<br /> | '''Crystal Structure of p38 Alpha in Complex with a Selective Pyridazine Inhibitor'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Novel potent trisubstituted pyridazine inhibitors of p38 MAP (mitogen | + | 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== | ==About this Structure== | ||
| - | 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 SO4 and 6NP 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:// | + | 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]. |
==Reference== | ==Reference== | ||
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[[Category: Tamayo, N.]] | [[Category: Tamayo, N.]] | ||
[[Category: Tudor, Y.]] | [[Category: Tudor, Y.]] | ||
| - | [[Category: Wong, M | + | [[Category: Wong, M L.]] |
[[Category: Yu, V.]] | [[Category: Yu, V.]] | ||
[[Category: 6NP]] | [[Category: 6NP]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:08:05 2008'' |
Revision as of 14:08, 21 February 2008
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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 with and as ligands. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 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 Feb 21 16:08:05 2008
Categories: Homo sapiens | Non-specific serine/threonine protein kinase | Single protein | Dominguez, C. | Goldberg, M. | Harvey, T. | Henkle, B. | Hungate, R. | Jang, G. | Li, V. | Liao, H. | Middelton, S. | Powers, D. | Syed, R. | Tamayo, N. | Tudor, Y. | Wong, M L. | Yu, V. | 6NP | SO4 | Transferase
