3b6h

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[[Image:3b6h.jpg|left|200px]]
[[Image:3b6h.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 3b6h |SIZE=350|CAPTION= <scene name='initialview01'>3b6h</scene>, resolution 1.62&Aring;
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The line below this paragraph, containing "STRUCTURE_3b6h", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Bog+Binding+Site+For+Residue+A+701'>AC1</scene>, <scene name='pdbsite=AC2:Bog+Binding+Site+For+Residue+B+702'>AC2</scene>, <scene name='pdbsite=AC3:Mxd+Binding+Site+For+Residue+A+551'>AC3</scene>, <scene name='pdbsite=AC4:Hem+Binding+Site+For+Residue+A+600'>AC4</scene>, <scene name='pdbsite=AC5:Mxd+Binding+Site+For+Residue+B+551'>AC5</scene> and <scene name='pdbsite=AC6:Hem+Binding+Site+For+Residue+B+600'>AC6</scene>
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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=BOG:B-OCTYLGLUCOSIDE'>BOG</scene>, <scene name='pdbligand=HEM:PROTOPORPHYRIN+IX+CONTAINING+FE'>HEM</scene>, <scene name='pdbligand=MXD:6-PIPERIDIN-1-YLPYRIMIDINE-2,4-DIAMINE+3-OXIDE'>MXD</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/Prostaglandin-I_synthase Prostaglandin-I synthase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=5.3.99.4 5.3.99.4] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= PTGIS, CYP8, CYP8A1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_3b6h| PDB=3b6h | SCENE= }}
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|RELATEDENTRY=[[2iag|2iag]], [[3b98|3B98]], [[3b99|3B99]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3b6h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3b6h OCA], [http://www.ebi.ac.uk/pdbsum/3b6h PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=3b6h RCSB]</span>
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}}
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'''Crystal structure of human prostacyclin synthase in complex with inhibitor minoxidil'''
'''Crystal structure of human prostacyclin synthase in complex with inhibitor minoxidil'''
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[[Category: Whitby, F G.]]
[[Category: Whitby, F G.]]
[[Category: Yeh, H C.]]
[[Category: Yeh, H C.]]
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[[Category: cyp8a1]]
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[[Category: Cyp8a1]]
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[[Category: cytochrome p450]]
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[[Category: Cytochrome p450]]
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[[Category: endoplasmic reticulum]]
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[[Category: Endoplasmic reticulum]]
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[[Category: enzyme-inhibitor complex]]
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[[Category: Enzyme-inhibitor complex]]
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[[Category: fatty acid biosynthesis]]
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[[Category: Fatty acid biosynthesis]]
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[[Category: heme]]
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[[Category: Heme]]
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[[Category: iron]]
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[[Category: Iron]]
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[[Category: isomerase]]
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[[Category: Isomerase]]
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[[Category: lipid synthesis]]
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[[Category: Lipid synthesis]]
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[[Category: membrane]]
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[[Category: Membrane]]
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[[Category: metal-binding]]
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[[Category: Metal-binding]]
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[[Category: polymorphism]]
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[[Category: Polymorphism]]
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[[Category: prostacyclin synthase]]
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[[Category: Prostacyclin synthase]]
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[[Category: prostaglandin biosynthesis]]
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[[Category: Prostaglandin biosynthesis]]
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[[Category: transmembrane]]
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[[Category: Transmembrane]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 20:26:14 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:23:28 2008''
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Revision as of 17:26, 4 May 2008

Image:3b6h.jpg

Template:STRUCTURE 3b6h

Crystal structure of human prostacyclin synthase in complex with inhibitor minoxidil


Overview

Prostacyclin synthase (PGIS) is a cytochrome P450 (P450) enzyme that catalyzes production of prostacyclin from prostaglandin H(2). PGIS is unusual in that it catalyzes an isomerization rather than a monooxygenation, which is typical of P450 enzymes. To understand the structural basis for prostacyclin biosynthesis in greater detail, we have determined the crystal structures of ligand-free, inhibitor (minoxidil)-bound and substrate analog U51605-bound PGIS. These structures demonstrate a stereo-specific substrate binding and suggest features of the enzyme that facilitate isomerization. Unlike most microsomal P450s, where large substrate-induced conformational changes take place at the distal side of the heme, conformational changes in PGIS are observed at the proximal side and in the heme itself. The conserved and extensive heme propionate-protein interactions seen in all other P450s, which are largely absent in the ligand-free PGIS, are recovered upon U51605 binding accompanied by water exclusion from the active site. In contrast, when minoxidil binds, the propionate-protein interactions are not recovered and water molecules are largely retained. These findings suggest that PGIS represents a divergent evolution of the P450 family, in which a heme barrier has evolved to ensure strict binding specificity for prostaglandin H(2), leading to a radical-mediated isomerization with high product fidelity. The U51605-bound structure also provides a view of the substrate entrance and product exit channels.

About this Structure

3B6H is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structures of Prostacyclin Synthase and Its Complexes with Substrate Analog and Inhibitor Reveal a Ligand-specific Heme Conformation Change., Li YC, Chiang CW, Yeh HC, Hsu PY, Whitby FG, Wang LH, Chan NL, J Biol Chem. 2008 Feb 1;283(5):2917-26. Epub 2007 Nov 21. PMID:18032380 Page seeded by OCA on Sun May 4 20:26:14 2008

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