1oyn

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[[Image:1oyn.gif|left|200px]]
[[Image:1oyn.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1oyn |SIZE=350|CAPTION= <scene name='initialview01'>1oyn</scene>, resolution 2.0&Aring;
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The line below this paragraph, containing "STRUCTURE_1oyn", 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=ROL:ROLIPRAM'>ROL</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/3',5'-cyclic-nucleotide_phosphodiesterase 3',5'-cyclic-nucleotide phosphodiesterase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.4.17 3.1.4.17] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= PDE4D2 ([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_1oyn| PDB=1oyn | SCENE= }}
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|RELATEDENTRY=[[1oym|1OYM]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1oyn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1oyn OCA], [http://www.ebi.ac.uk/pdbsum/1oyn PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1oyn RCSB]</span>
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}}
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'''Crystal structure of PDE4D2 in complex with (R,S)-rolipram'''
'''Crystal structure of PDE4D2 in complex with (R,S)-rolipram'''
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[[Category: Sun, Y.]]
[[Category: Sun, Y.]]
[[Category: Wang, H.]]
[[Category: Wang, H.]]
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[[Category: camp]]
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[[Category: Camp]]
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[[Category: pde]]
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[[Category: Pde]]
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[[Category: rolipram]]
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[[Category: Rolipram]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 04:26:23 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:52:13 2008''
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Revision as of 01:26, 3 May 2008

Image:1oyn.gif

Template:STRUCTURE 1oyn

Crystal structure of PDE4D2 in complex with (R,S)-rolipram


Overview

Selective inhibitors against the 11 families of cyclic nucleotide phosphodiesterases (PDEs) are used to treat various human diseases. How the inhibitors selectively bind the conserved PDE catalytic domains is unknown. The crystal structures of the PDE4D2 catalytic domain in complex with (R)- or (R,S)-rolipram suggest that inhibitor selectivity is determined by the chemical nature of amino acids and subtle conformational changes of the binding pockets. The conformational states of Gln369 in PDE4D2 may play a key role in inhibitor recognition. The corresponding Y329S mutation in PDE7 may lead to loss of the hydrogen bonds between rolipram and Gln369 and is thus a possible reason explaining PDE7's insensitivity to rolipram inhibition. Docking of the PDE5 inhibitor sildenafil into the PDE4 catalytic pocket further helps understand inhibitor selectivity.

About this Structure

1OYN is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Three-dimensional structures of PDE4D in complex with roliprams and implication on inhibitor selectivity., Huai Q, Wang H, Sun Y, Kim HY, Liu Y, Ke H, Structure. 2003 Jul;11(7):865-73. PMID:12842049 Page seeded by OCA on Sat May 3 04:26:23 2008

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