2p3g

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[[Image:2p3g.jpg|left|200px]]
[[Image:2p3g.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2p3g |SIZE=350|CAPTION= <scene name='initialview01'>2p3g</scene>, resolution 3.800&Aring;
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The line below this paragraph, containing "STRUCTURE_2p3g", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:F10+Binding+Site+For+Residue+X+401'>AC1</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=F10:2-[2-(2-FLUOROPHENYL)PYRIDIN-4-YL]-1,5,6,7-TETRAHYDRO-4H-PYRROLO[3,2-C]PYRIDIN-4-ONE'>F10</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[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] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= MAPKAPK2 ([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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|DOMAIN=
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{{STRUCTURE_2p3g| PDB=2p3g | SCENE= }}
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|RELATEDENTRY=[[1kwp|1KWP]], [[1ny3|1NY3]], [[1nxk|1NXK]], [[2onl|2ONL]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2p3g FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2p3g OCA], [http://www.ebi.ac.uk/pdbsum/2p3g PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2p3g RCSB]</span>
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}}
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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'''
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[[Category: Caspers, N.]]
[[Category: Caspers, N.]]
[[Category: Kurumbail, R G.]]
[[Category: Kurumbail, R G.]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: kinase domain]]
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[[Category: Kinase domain]]
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[[Category: map kinase]]
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[[Category: Map kinase]]
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[[Category: mk-2]]
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[[Category: Mk-2]]
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[[Category: mk2]]
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[[Category: Mk2]]
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[[Category: serine/threonine kinase]]
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[[Category: Serine/threonine kinase]]
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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 12:16:04 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:28:35 2008''
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Revision as of 09:16, 4 May 2008

Image:2p3g.jpg

Template:STRUCTURE 2p3g

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. 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 Sun May 4 12:16:04 2008

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