1oz1
From Proteopedia
(New page: 200px<br /> <applet load="1oz1" size="450" color="white" frame="true" align="right" spinBox="true" caption="1oz1, resolution 2.10Å" /> '''P38 MITOGEN-ACTIVAT...) |
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| - | [[Image:1oz1. | + | [[Image:1oz1.jpg|left|200px]]<br /><applet load="1oz1" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="1oz1, resolution 2.10Å" /> | caption="1oz1, resolution 2.10Å" /> | ||
'''P38 MITOGEN-ACTIVATED KINASE IN COMPLEX WITH 4-AZAINDOLE INHIBITOR'''<br /> | '''P38 MITOGEN-ACTIVATED KINASE IN COMPLEX WITH 4-AZAINDOLE INHIBITOR'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1OZ1 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 FPH as [http://en.wikipedia.org/wiki/ligand ligand]. 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:// | + | 1OZ1 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=FPH:'>FPH</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. 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=1OZ1 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: ser/thr protein kinase]] | [[Category: ser/thr protein kinase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:37:37 2008'' |
Revision as of 14:37, 15 February 2008
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P38 MITOGEN-ACTIVATED KINASE IN COMPLEX WITH 4-AZAINDOLE INHIBITOR
Overview
Inhibition of the biosynthesis of proinflammatory cytokines such as tumor, necrosis factor and interleukin-1 via p38 has been an approach toward the, development of a disease modifying agent for the treatment of chronic, inflammation and autoimmune diseases. The development of a new core, structure of p38 inhibitors, 3-(4-fluorophenyl)-2-(pyridin-4-yl)-1H-pyrrolo[3,2-b] pyridine, is, described. X-ray crystallographic data of the lead bound to the active, site of p38 was used to guide the optimization of the series. Specific, focus was placed on modulating the physical properties of the core while, maintaining potent inhibition of p38. These efforts identified 42c as a, potent inhibitor of p38, which also possessed the required physical, properties worthy of advanced studies.
About this Structure
1OZ1 is a Single protein structure of sequence from Homo sapiens with as ligand. 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 4-azaindoles as inhibitors of p38 MAP kinase., Trejo A, Arzeno H, Browner M, Chanda S, Cheng S, Comer DD, Dalrymple SA, Dunten P, Lafargue J, Lovejoy B, Freire-Moar J, Lim J, Mcintosh J, Miller J, Papp E, Reuter D, Roberts R, Sanpablo F, Saunders J, Song K, Villasenor A, Warren SD, Welch M, Weller P, Whiteley PE, Zeng L, Goldstein DM, J Med Chem. 2003 Oct 23;46(22):4702-13. PMID:14561090
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