2p3g
From Proteopedia
(New page: 200px<br /> <applet load="2p3g" size="450" color="white" frame="true" align="right" spinBox="true" caption="2p3g, resolution 3.800Å" /> '''Crystal structure ...) |
|||
| Line 1: | Line 1: | ||
| - | [[Image:2p3g. | + | [[Image:2p3g.jpg|left|200px]]<br /><applet load="2p3g" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2p3g" size=" | + | |
caption="2p3g, resolution 3.800Å" /> | caption="2p3g, resolution 3.800Å" /> | ||
'''Crystal structure of a pyrrolopyridine inhibitor bound to MAPKAP Kinase-2'''<br /> | '''Crystal structure of a pyrrolopyridine inhibitor bound to MAPKAP Kinase-2'''<br /> | ||
| Line 8: | Line 7: | ||
==About this Structure== | ==About this Structure== | ||
| - | 2P3G 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 F10 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:// | + | 2P3G 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=F10:'>F10</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=2P3G OCA]. |
==Reference== | ==Reference== | ||
| Line 25: | Line 24: | ||
[[Category: serine/threonine kinase]] | [[Category: serine/threonine kinase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 14:55:39 2008'' |
Revision as of 12:55, 23 January 2008
|
Crystal structure of a pyrrolopyridine inhibitor bound to MAPKAP Kinase-2
Overview
A new class of potent kinase inhibitors selective for mitogen-activated, protein kinase-activated protein kinase 2 (MAPKAP-K2 or MK-2) for the, treatment of rheumatoid arthritis has been prepared and evaluated. These, inhibitors have IC50 values as low as 10 nM against the target and have, good selectivity profiles against a number of kinases including CDK2, ERK, JNK, and p38. These MK-2 inhibitors have been shown to suppress TNFalpha, production in U397 cells and to be efficacious in an acute inflammation, model. The structure-activity relationships of this series, the, selectivity for MK-2 and their activity in both in vitro and in vivo, models are discussed. The observed selectivity is discussed with the aid, of an MK-2/inhibitor crystal structure.
About this Structure
2P3G 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
Pyrrolopyridine Inhibitors of Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MK-2)., Anderson DR, Meyers MJ, Vernier WF, Mahoney MW, Kurumbail RG, Caspers N, Poda GI, Schindler JF, Reitz DB, Mourey RJ, J Med Chem. 2007 May 31;50(11):2647-54. Epub 2007 May 5. PMID:17480064
Page seeded by OCA on Wed Jan 23 14:55:39 2008
