1vaf

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[[Image:1vaf.gif|left|200px]]
[[Image:1vaf.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1vaf |SIZE=350|CAPTION= <scene name='initialview01'>1vaf</scene>, resolution 2.9&Aring;
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The line below this paragraph, containing "STRUCTURE_1vaf", 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=ARR:N-(4-{2-[(3-CHLOROBENZYL)AMINO]ETHYL}PHENYL)THIOPHENE-2-CARBOXIMIDAMIDE'>ARR</scene>, <scene name='pdbligand=H4B:5,6,7,8-TETRAHYDROBIOPTERIN'>H4B</scene>, <scene name='pdbligand=HEM:PROTOPORPHYRIN+IX+CONTAINING+FE'>HEM</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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_1vaf| PDB=1vaf | SCENE= }}
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|RELATEDENTRY=[[1qw4|1QW4]], [[1qw5|1QW5]], [[1qw6|1QW6]], [[1qwc|1QWC]], [[1vag|1VAG]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1vaf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1vaf OCA], [http://www.ebi.ac.uk/pdbsum/1vaf PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1vaf RCSB]</span>
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}}
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'''Inducible nitric oxide synthase oxygenase domain complexed with the inhibitor AR-R17477'''
'''Inducible nitric oxide synthase oxygenase domain complexed with the inhibitor AR-R17477'''
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[[Category: Schlichting, I.]]
[[Category: Schlichting, I.]]
[[Category: Vasan, R.]]
[[Category: Vasan, R.]]
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[[Category: murine inosoxy inhibitor complex]]
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[[Category: Murine inosoxy inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 12:17:58 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:21:42 2008''
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Revision as of 09:17, 3 May 2008

Image:1vaf.gif

Template:STRUCTURE 1vaf

Inducible nitric oxide synthase oxygenase domain complexed with the inhibitor AR-R17477


Overview

The high level of amino acid conservation and structural similarity of the substrate-binding sites of the oxygenase domains of the nitric oxide synthase (NOS) isoforms (eNOSoxy, iNOSoxy, nNOSoxy) make the interpretation of the structural basis of inhibitor isoform specificity a challenge, and provide few clues for the design of new selective compounds. Crystal structures of iNOSoxy and nNOSoxy complexed with the neuronal NOS-specific inhibitor AR-R17447 suggest that specificity is provided by the interaction of the chlorophenyl group with an isoform-unique substrate access channel residue (L337 in rat neuronal NOS, N115 in mouse inducible NOS). This is confirmed by biochemical analysis of site-directed mutants. Inhibitors combining guanidinium-like structural motifs with long chains specifically targeting this residue are good candidates for rational isoform-specific drug design. Based on this finding, modifications of AR-R17447 to improve the specificity for the human isoforms are suggested.

About this Structure

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

Reference

Structures of nitric oxide synthase isoforms complexed with the inhibitor AR-R17477 suggest a rational basis for specificity and inhibitor design., Fedorov R, Vasan R, Ghosh DK, Schlichting I, Proc Natl Acad Sci U S A. 2004 Apr 20;101(16):5892-7. Epub 2004 Apr 7. PMID:15071192 Page seeded by OCA on Sat May 3 12:17:58 2008

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