1oz1

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{{STRUCTURE_1oz1| PDB=1oz1 | SCENE= }}
{{STRUCTURE_1oz1| PDB=1oz1 | SCENE= }}
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'''P38 MITOGEN-ACTIVATED KINASE IN COMPLEX WITH 4-AZAINDOLE INHIBITOR'''
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===P38 MITOGEN-ACTIVATED KINASE IN COMPLEX WITH 4-AZAINDOLE INHIBITOR===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 14561090 is the PubMed ID number.
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{{ABSTRACT_PUBMED_14561090}}
==About this Structure==
==About this Structure==
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[[Category: Villasenor, A.]]
[[Category: Villasenor, A.]]
[[Category: Ser/thr protein kinase]]
[[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 Tue Jul 29 16:35:20 2008''

Revision as of 13:35, 29 July 2008

Image:1oz1.png

Template:STRUCTURE 1oz1

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

Template:ABSTRACT PUBMED 14561090

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

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