2p3g: Difference between revisions

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[[Image:2p3g.~~jpg~~|left|200px]]

[[Image:2p3g.png|left|200px]]

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~~'''~~Crystal structure of a pyrrolopyridine inhibitor bound to MAPKAP Kinase-2~~'''~~

===Crystal structure of a pyrrolopyridine inhibitor bound to MAPKAP Kinase-2===

~~==Overview==~~

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~~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.~~

The line below this paragraph, {{ABSTRACT_PUBMED_17480064}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 17480064 is the PubMed ID number.

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==About this Structure==

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[[Category: Serine/threonine kinase]]

[[Category: Transferase]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sun May 4 12~~:16~~:04~~ 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 13:04:16 2008''

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-[[Image:2p3g.jpg|left|200px]]
+{{Seed}}
+[[Image:2p3g.png|left|200px]]
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 {{STRUCTURE_2p3g|  PDB=2p3g  |  SCENE=  }}
-'''Crystal structure of a pyrrolopyridine inhibitor bound to MAPKAP Kinase-2'''
+===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.
+The line below this paragraph, {{ABSTRACT_PUBMED_17480064}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 17480064 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_17480064}}
 ==About this Structure==
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 [[Category: Serine/threonine kinase]]
 [[Category: Transferase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 12:16:04 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 13:04:16 2008''