2pzy

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[[Image:2pzy.jpg|left|200px]]
[[Image:2pzy.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2pzy |SIZE=350|CAPTION= <scene name='initialview01'>2pzy</scene>, resolution 2.900&Aring;
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The line below this paragraph, containing "STRUCTURE_2pzy", creates the "Structure Box" on the page.
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|SITE=
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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=B18:(4R)-N-[4-({[2-(DIMETHYLAMINO)ETHYL]AMINO}CARBONYL)-1,3-THIAZOL-2-YL]-4-METHYL-1-OXO-2,3,4,9-TETRAHYDRO-1H-BETA-CARBOLINE-6-CARBOXAMIDE'>B18</scene>, <scene name='pdbligand=STU:STAUROSPORINE'>STU</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_2pzy| PDB=2pzy | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2pzy FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2pzy OCA], [http://www.ebi.ac.uk/pdbsum/2pzy PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2pzy RCSB]</span>
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}}
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'''Structure of MK2 Complexed with Compound 76'''
'''Structure of MK2 Complexed with Compound 76'''
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[[Category: White, A.]]
[[Category: White, A.]]
[[Category: Wu, J P.]]
[[Category: Wu, J P.]]
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[[Category: mk2]]
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[[Category: Mk2]]
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[[Category: protein kinase]]
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[[Category: Protein 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 14:05:10 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:42:52 2008''
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Revision as of 11:05, 4 May 2008

Image:2pzy.jpg

Template:STRUCTURE 2pzy

Structure of MK2 Complexed with Compound 76


Overview

The discovery of a series of potent, carboline-based MK2 inhibitors is described. These compounds inhibit MK2 with IC50s as low as 10 nM, as measured in a DELFIA assay. An X-ray crystal structure reveals that they bind in a region near the p-loop and the hinge region of MK2a.

About this Structure

2PZY is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

The discovery of carboline analogs as potent MAPKAP-K2 inhibitors., Wu JP, Wang J, Abeywardane A, Andersen D, Emmanuel M, Gautschi E, Goldberg DR, Kashem MA, Lukas S, Mao W, Martin L, Morwick T, Moss N, Pargellis C, Patel UR, Patnaude L, Peet GW, Skow D, Snow RJ, Ward Y, Werneburg B, White A, Bioorg Med Chem Lett. 2007 Aug 15;17(16):4664-9. Epub 2007 Jun 7. PMID:17576063 Page seeded by OCA on Sun May 4 14:05:10 2008

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OCA

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