2oji

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[[Image:2oji.gif|left|200px]]
[[Image:2oji.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2oji |SIZE=350|CAPTION= <scene name='initialview01'>2oji</scene>, resolution 2.600&Aring;
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The line below this paragraph, containing "STRUCTURE_2oji", 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=33A:N-BENZYL-4-[4-(3-CHLOROPHENYL)-1H-PYRAZOL-3-YL]-1H-PYRROLE-2-CARBOXAMIDE'>33A</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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/Mitogen-activated_protein_kinase Mitogen-activated protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.24 2.7.11.24] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= MAPK1, ERK2, PRKM1 ([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_2oji| PDB=2oji | SCENE= }}
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|RELATEDENTRY=[[2ojg|2OJG]], [[2ojj|2OJJ]], [[2ok1|2OK1]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2oji FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2oji OCA], [http://www.ebi.ac.uk/pdbsum/2oji PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2oji RCSB]</span>
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}}
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'''Crystal structure of ERK2 in complex with N-benzyl-4-(4-(3-chlorophenyl)-1H-pyrazol-3-yl)-1H-pyrrole-2-carboxamide'''
'''Crystal structure of ERK2 in complex with N-benzyl-4-(4-(3-chlorophenyl)-1H-pyrazol-3-yl)-1H-pyrrole-2-carboxamide'''
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[[Category: Jacobs, M D.]]
[[Category: Jacobs, M D.]]
[[Category: Xie, X.]]
[[Category: Xie, X.]]
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[[Category: kinase inhibitor]]
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[[Category: Kinase inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:02:34 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:18:40 2008''
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Revision as of 08:02, 4 May 2008

Image:2oji.gif

Template:STRUCTURE 2oji

Crystal structure of ERK2 in complex with N-benzyl-4-(4-(3-chlorophenyl)-1H-pyrazol-3-yl)-1H-pyrrole-2-carboxamide


Overview

The Ras/Raf/MEK/ERK signal transduction is a key oncogenic pathway implicated in a variety of human cancers. We have identified a novel series of pyrazolylpyrroles as inhibitors of ERK. Aided by the discovery of two distinct binding modes for the pyrazolylpyrrole scaffold, structure-guided optimization culminated in the discovery of 6p, a potent and selective inhibitor of ERK.

About this Structure

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

Reference

Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors., Aronov AM, Baker C, Bemis GW, Cao J, Chen G, Ford PJ, Germann UA, Green J, Hale MR, Jacobs M, Janetka JW, Maltais F, Martinez-Botella G, Namchuk MN, Straub J, Tang Q, Xie X, J Med Chem. 2007 Mar 22;50(6):1280-7. Epub 2007 Feb 15. PMID:17300186 Page seeded by OCA on Sun May 4 11:02:34 2008

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OCA

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