4nos
From Proteopedia
(New page: 200px<br /> <applet load="4nos" size="450" color="white" frame="true" align="right" spinBox="true" caption="4nos, resolution 2.250Å" /> '''HUMAN INDUCIBLE NI...) |
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- | [[Image:4nos.gif|left|200px]]<br /> | + | [[Image:4nos.gif|left|200px]]<br /><applet load="4nos" size="350" color="white" frame="true" align="right" spinBox="true" |
- | <applet load="4nos" size=" | + | |
caption="4nos, resolution 2.250Å" /> | caption="4nos, resolution 2.250Å" /> | ||
'''HUMAN INDUCIBLE NITRIC OXIDE SYNTHASE WITH INHIBITOR'''<br /> | '''HUMAN INDUCIBLE NITRIC OXIDE SYNTHASE WITH INHIBITOR'''<br /> | ||
==Overview== | ==Overview== | ||
- | Crystal structures of human endothelial nitric oxide synthase (eNOS) and | + | Crystal structures of human endothelial nitric oxide synthase (eNOS) and human inducible NOS (iNOS) catalytic domains were solved in complex with the arginine substrate and an inhibitor S-ethylisothiourea (SEITU), respectively. The small molecules bind in a narrow cleft within the larger active-site cavity containing heme and tetrahydrobiopterin. Both are hydrogen-bonded to a conserved glutamate (eNOS E361, iNOS E377). The active-site residues of iNOS and eNOS are nearly identical. Nevertheless, structural comparisons provide a basis for design of isozyme-selective inhibitors. The high-resolution, refined structures of eNOS (2.4 A resolution) and iNOS (2.25 A resolution) reveal an unexpected structural zinc situated at the intermolecular interface and coordinated by four cysteines, two from each monomer. |
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
- | 4NOS is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with ZN, HEM, H2B, ITU and H4B as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http:// | + | 4NOS is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=ZN:'>ZN</scene>, <scene name='pdbligand=HEM:'>HEM</scene>, <scene name='pdbligand=H2B:'>H2B</scene>, <scene name='pdbligand=ITU:'>ITU</scene> and <scene name='pdbligand=H4B:'>H4B</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4NOS OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Nitric-oxide synthase]] | [[Category: Nitric-oxide synthase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
- | [[Category: Fischmann, T | + | [[Category: Fischmann, T O.]] |
- | [[Category: Weber, P | + | [[Category: Weber, P C.]] |
[[Category: H2B]] | [[Category: H2B]] | ||
[[Category: H4B]] | [[Category: H4B]] | ||
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[[Category: zns4]] | [[Category: zns4]] | ||
- | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 19:13:52 2008'' |
Revision as of 17:13, 21 February 2008
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HUMAN INDUCIBLE NITRIC OXIDE SYNTHASE WITH INHIBITOR
Contents |
Overview
Crystal structures of human endothelial nitric oxide synthase (eNOS) and human inducible NOS (iNOS) catalytic domains were solved in complex with the arginine substrate and an inhibitor S-ethylisothiourea (SEITU), respectively. The small molecules bind in a narrow cleft within the larger active-site cavity containing heme and tetrahydrobiopterin. Both are hydrogen-bonded to a conserved glutamate (eNOS E361, iNOS E377). The active-site residues of iNOS and eNOS are nearly identical. Nevertheless, structural comparisons provide a basis for design of isozyme-selective inhibitors. The high-resolution, refined structures of eNOS (2.4 A resolution) and iNOS (2.25 A resolution) reveal an unexpected structural zinc situated at the intermolecular interface and coordinated by four cysteines, two from each monomer.
Disease
Known diseases associated with this structure: Hypertension, susceptibility to OMIM:[163730], Malaria, resistance to OMIM:[163730]
About this Structure
4NOS is a Single protein structure of sequence from Homo sapiens with , , , and as ligands. Active as Nitric-oxide synthase, with EC number 1.14.13.39 Full crystallographic information is available from OCA.
Reference
Structural characterization of nitric oxide synthase isoforms reveals striking active-site conservation., Fischmann TO, Hruza A, Niu XD, Fossetta JD, Lunn CA, Dolphin E, Prongay AJ, Reichert P, Lundell DJ, Narula SK, Weber PC, Nat Struct Biol. 1999 Mar;6(3):233-42. PMID:10074942
Page seeded by OCA on Thu Feb 21 19:13:52 2008
Categories: Homo sapiens | Nitric-oxide synthase | Single protein | Fischmann, T O. | Weber, P C. | H2B | H4B | HEM | ITU | ZN | Human | L-arginine monooxygenase | Nitric oxide | Zns4