1oz1

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[[Image:1oz1.jpg|left|200px]]
[[Image:1oz1.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1oz1 |SIZE=350|CAPTION= <scene name='initialview01'>1oz1</scene>, resolution 2.10&Aring;
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The line below this paragraph, containing "STRUCTURE_1oz1", 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=FPH:3-(4-FLUOROPHENYL)-2-PYRIDIN-4-YL-1H-PYRROLO[3,2-B]PYRIDIN-1-OL'>FPH</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= MAPK14 OR CSBP1 OR CSBP2 OR CSBP OR MXI2 ([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_1oz1| PDB=1oz1 | 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=1oz1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1oz1 OCA], [http://www.ebi.ac.uk/pdbsum/1oz1 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1oz1 RCSB]</span>
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}}
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'''P38 MITOGEN-ACTIVATED KINASE IN COMPLEX WITH 4-AZAINDOLE INHIBITOR'''
'''P38 MITOGEN-ACTIVATED KINASE IN COMPLEX WITH 4-AZAINDOLE INHIBITOR'''
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[[Category: Lovejoy, B.]]
[[Category: Lovejoy, B.]]
[[Category: Villasenor, A.]]
[[Category: Villasenor, A.]]
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[[Category: ser/thr protein kinase]]
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[[Category: Ser/thr protein kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 04:27:15 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:52:26 2008''
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Revision as of 01:27, 3 May 2008

Image:1oz1.jpg

Template:STRUCTURE 1oz1

P38 MITOGEN-ACTIVATED KINASE IN COMPLEX WITH 4-AZAINDOLE INHIBITOR


Overview

Inhibition of the biosynthesis of proinflammatory cytokines such as tumor necrosis factor and interleukin-1 via p38 has been an approach toward the development of a disease modifying agent for the treatment of chronic inflammation and autoimmune diseases. The development of a new core structure of p38 inhibitors, 3-(4-fluorophenyl)-2-(pyridin-4-yl)-1H-pyrrolo[3,2-b] pyridine, is described. X-ray crystallographic data of the lead bound to the active site of p38 was used to guide the optimization of the series. Specific focus was placed on modulating the physical properties of the core while maintaining potent inhibition of p38. These efforts identified 42c as a potent inhibitor of p38, which also possessed the required physical properties worthy of advanced studies.

About this Structure

1OZ1 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Design and synthesis of 4-azaindoles as inhibitors of p38 MAP kinase., Trejo A, Arzeno H, Browner M, Chanda S, Cheng S, Comer DD, Dalrymple SA, Dunten P, Lafargue J, Lovejoy B, Freire-Moar J, Lim J, Mcintosh J, Miller J, Papp E, Reuter D, Roberts R, Sanpablo F, Saunders J, Song K, Villasenor A, Warren SD, Welch M, Weller P, Whiteley PE, Zeng L, Goldstein DM, J Med Chem. 2003 Oct 23;46(22):4702-13. PMID:14561090 Page seeded by OCA on Sat May 3 04:27:15 2008

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