2h96

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[[Image:2h96.gif|left|200px]]
[[Image:2h96.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2h96 |SIZE=350|CAPTION= <scene name='initialview01'>2h96</scene>, resolution 3.00&Aring;
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The line below this paragraph, containing "STRUCTURE_2h96", 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=893:5-CYANO-N-(2,5-DIMETHOXYBENZYL)-6-ETHOXYPYRIDINE-2-CARBOXAMIDE'>893</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</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= MAPK8, JNK1, PRKM8 ([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_2h96| PDB=2h96 | SCENE= }}
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|RELATEDENTRY=[[2g01|2g01]], [[2gmx|2gmx]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2h96 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2h96 OCA], [http://www.ebi.ac.uk/pdbsum/2h96 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2h96 RCSB]</span>
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}}
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'''Discovery of Potent, Highly Selective, and Orally Bioavailable Pyridine Carboxamide C-jun NH2-terminal Kinase Inhibitors'''
'''Discovery of Potent, Highly Selective, and Orally Bioavailable Pyridine Carboxamide C-jun NH2-terminal Kinase Inhibitors'''
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[[Category: Protein complex]]
[[Category: Protein complex]]
[[Category: Abad-Zapatero, C.]]
[[Category: Abad-Zapatero, C.]]
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[[Category: c-jun n-terminal kinase]]
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[[Category: C-jun n-terminal kinase]]
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[[Category: jnk1]]
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[[Category: Jnk1]]
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[[Category: protein kinase jnk1 inhibitor]]
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[[Category: Protein kinase jnk1 inhibitor]]
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[[Category: pyridine carboxamide inhibitor]]
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[[Category: Pyridine carboxamide inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 06:00:42 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:27:12 2008''
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Revision as of 03:00, 4 May 2008

Template:STRUCTURE 2h96

Discovery of Potent, Highly Selective, and Orally Bioavailable Pyridine Carboxamide C-jun NH2-terminal Kinase Inhibitors


Overview

C-Jun NH2 terminal kinases (JNKs) are important cell signaling enzymes. JNK1 plays a central role in linking obesity and insulin resistance. JNK2 and JNK3 may be involved in inflammatory and neurological disorders, respectively. Small-molecule JNK inhibitors could be valuable tools to study the therapeutic benefits of inhibiting these enzymes and as leads for potential drugs targeting JNKs. In this report, we disclose a series of potent and highly selective JNK inhibitors with good pharmacokinetic profiles.

About this Structure

2H96 is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors., Zhao H, Serby MD, Xin Z, Szczepankiewicz BG, Liu M, Kosogof C, Liu B, Nelson LT, Johnson EF, Wang S, Pederson T, Gum RJ, Clampit JE, Haasch DL, Abad-Zapatero C, Fry EH, Rondinone C, Trevillyan JM, Sham HL, Liu G, J Med Chem. 2006 Jul 27;49(15):4455-8. PMID:16854050 Page seeded by OCA on Sun May 4 06:00:42 2008

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