2oro

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{{STRUCTURE_2oro| PDB=2oro | SCENE= }}
{{STRUCTURE_2oro| PDB=2oro | SCENE= }}
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'''Murine inducible nitric oxide synthase oxygenase domain (delta 114) (r)-1-(2-imidazol-1-yl-6-methyl-pyrimidin-4-yl)-pyrrolidine-2-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-amide complex'''
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===Murine inducible nitric oxide synthase oxygenase domain (delta 114) (r)-1-(2-imidazol-1-yl-6-methyl-pyrimidin-4-yl)-pyrrolidine-2-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-amide complex===
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==Overview==
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By the screening of a combinatorial library for inhibitors of nitric oxide (NO) formation by the inducible isoform of nitric oxide synthase (iNOS) using a whole-cell assay, 2-(imidazol-1-yl)pyrimidines were identified. Compounds were found to inhibit the dimerization of iNOS monomers, thus preventing the formation of the dimeric, active form of the enzyme. Optimization led to the selection of the potent, selective, and orally available iNOS dimerization inhibitor, 21b, which significantly ameliorated adjuvant-induced arthritis in a rat model. Analysis of the crystal structure of the 21b--iNOS monomer complex provided a rationalization for both the SAR and the mechanism by which 21b blocks the formation of the protein--protein interaction present in the dimeric form of iNOS.
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(as it appears on PubMed at http://www.pubmed.gov), where 17315988 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17315988}}
==About this Structure==
==About this Structure==
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[[Category: Nitric oxide]]
[[Category: Nitric oxide]]
[[Category: No]]
[[Category: No]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:31:53 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 07:47:40 2008''

Revision as of 04:47, 28 July 2008

Image:2oro.png

Template:STRUCTURE 2oro

Murine inducible nitric oxide synthase oxygenase domain (delta 114) (r)-1-(2-imidazol-1-yl-6-methyl-pyrimidin-4-yl)-pyrrolidine-2-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-amide complex

Template:ABSTRACT PUBMED 17315988

About this Structure

2ORO is a Single protein structure of sequence from Mus musculus. Full crystallographic information is available from OCA.

Reference

Design, synthesis, and activity of 2-imidazol-1-ylpyrimidine derived inducible nitric oxide synthase dimerization inhibitors., Davey DD, Adler M, Arnaiz D, Eagen K, Erickson S, Guilford W, Kenrick M, Morrissey MM, Ohlmeyer M, Pan G, Paradkar VM, Parkinson J, Polokoff M, Saionz K, Santos C, Subramanyam B, Vergona R, Wei RG, Whitlow M, Ye B, Zhao ZS, Devlin JJ, Phillips G, J Med Chem. 2007 Mar 22;50(6):1146-57. Epub 2007 Feb 23. PMID:17315988

Page seeded by OCA on Mon Jul 28 07:47:40 2008

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