1r35

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[[Image:1r35.jpg|left|200px]]
[[Image:1r35.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1r35 |SIZE=350|CAPTION= <scene name='initialview01'>1r35</scene>, resolution 2.30&Aring;
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The line below this paragraph, containing "STRUCTURE_1r35", 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=H4B:5,6,7,8-TETRAHYDROBIOPTERIN'>H4B</scene>, <scene name='pdbligand=HEM:PROTOPORPHYRIN+IX+CONTAINING+FE'>HEM</scene>, <scene name='pdbligand=I58:4R-FLUORO-N6-ETHANIMIDOYL-L-LYSINE'>I58</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/Nitric-oxide_synthase Nitric-oxide synthase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.14.13.39 1.14.13.39] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= NOS2, INOSL ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 Mus musculus])
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-->
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|DOMAIN=
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{{STRUCTURE_1r35| PDB=1r35 | 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=1r35 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1r35 OCA], [http://www.ebi.ac.uk/pdbsum/1r35 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1r35 RCSB]</span>
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}}
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'''MURINE INDUCIBLE NITRIC OXIDE SYNTHASE OXYGENASE DIMER, TETRAHYDROBIOPTERIN AND 4R-FLUORO-N6-ETHANIMIDOYL-L-LYSINE'''
'''MURINE INDUCIBLE NITRIC OXIDE SYNTHASE OXYGENASE DIMER, TETRAHYDROBIOPTERIN AND 4R-FLUORO-N6-ETHANIMIDOYL-L-LYSINE'''
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[[Category: Stallings, W C.]]
[[Category: Stallings, W C.]]
[[Category: Stevens, A M.]]
[[Category: Stevens, A M.]]
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[[Category: dimer]]
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[[Category: Dimer]]
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[[Category: h4b]]
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[[Category: H4b]]
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[[Category: heme]]
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[[Category: Heme]]
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[[Category: intermediate]]
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[[Category: Intermediate]]
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[[Category: nitric oxide monooxygenase]]
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[[Category: Nitric oxide monooxygenase]]
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[[Category: pterin]]
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[[Category: Pterin]]
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[[Category: tetrahydrobiopterin]]
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[[Category: Tetrahydrobiopterin]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 07:01:06 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:22:37 2008''
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Revision as of 04:01, 3 May 2008

Image:1r35.jpg

Template:STRUCTURE 1r35

MURINE INDUCIBLE NITRIC OXIDE SYNTHASE OXYGENASE DIMER, TETRAHYDROBIOPTERIN AND 4R-FLUORO-N6-ETHANIMIDOYL-L-LYSINE


Overview

In the literature, the introduction of fluorine into bioactive molecules has been known to enhance the biological activity relative to the parent molecule. Described in this article is the synthesis of 4R-fluoro-L-NIL (12) and 4,4-difluoro-L-NIL (23) as part of our iNOS program. Both 12 and 23 were found to be selective iNOS inhibitors as shown in Table 2 below. Secondarily, methodology to synthesize orthogonally protected 4-fluoro-L-lysine and 4,4-difluoro-L-lysine has been developed.

About this Structure

1R35 is a Single protein structure of sequence from Mus musculus. Full crystallographic information is available from OCA.

Reference

4-Fluorinated L-lysine analogs as selective i-NOS inhibitors: methodology for introducing fluorine into the lysine side chain., Hallinan EA, Kramer SW, Houdek SC, Moore WM, Jerome GM, Spangler DP, Stevens AM, Shieh HS, Manning PT, Pitzele BS, Org Biomol Chem. 2003 Oct 21;1(20):3527-34. PMID:14599013 Page seeded by OCA on Sat May 3 07:01:06 2008

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OCA

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