1ro6

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[[Image:1ro6.gif|left|200px]]
[[Image:1ro6.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1ro6 |SIZE=350|CAPTION= <scene name='initialview01'>1ro6</scene>, resolution 2.0&Aring;
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The line below this paragraph, containing "STRUCTURE_1ro6", 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=ARS:ARSENIC'>ARS</scene>, <scene name='pdbligand=MN:MANGANESE+(II)+ION'>MN</scene>, <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= PDE4B ([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_1ro6| PDB=1ro6 | SCENE= }}
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|RELATEDENTRY=[[1ro9|1RO9]], [[1ror|1ROR]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1ro6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1ro6 OCA], [http://www.ebi.ac.uk/pdbsum/1ro6 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1ro6 RCSB]</span>
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}}
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'''Crystal structure of PDE4B2B complexed with Rolipram (R & S)'''
'''Crystal structure of PDE4B2B complexed with Rolipram (R & S)'''
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[[Category: Vanderwall, D E.]]
[[Category: Vanderwall, D E.]]
[[Category: Xu, R X.]]
[[Category: Xu, R X.]]
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[[Category: crystal]]
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[[Category: Crystal]]
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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 07:43:12 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:30:48 2008''
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Revision as of 04:43, 3 May 2008

Image:1ro6.gif

Template:STRUCTURE 1ro6

Crystal structure of PDE4B2B complexed with Rolipram (R & S)


Overview

Phosphodiesterase catalyzes the hydrolysis of the intracellular second messenger 3',5'-cyclic AMP (cAMP) into the corresponding 5'-nucleotide. Phosphodiesterase 4 (PDE4), the major cAMP-specific PDE in inflammatory and immune cells, is an attractive target for the treatment of asthma and COPD. We have determined crystal structures of the catalytic domain of PDE4B complexed with AMP (2.0 A), 8-Br-AMP (2.13 A) and the potent inhibitor rolipram (2.0 A). All the ligands bind in the same hydrophobic pocket and can interact directly with the active site metal ions. The identity of these metal ions was examined using X-ray anomalous difference data. The structure of the AMP complex confirms the location of the catalytic site and allowed us to speculate about the detailed mechanism of catalysis. The high-resolution structures provided the experimental insight into the nucleotide selectivity of phosphodiesterase. 8-Br-AMP binds in the syn conformation to the enzyme and demonstrates an alternative nucleotide-binding mode. Rolipram occupies much of the AMP-binding site and forms two hydrogen bonds with Gln443 similar to the nucleotides.

About this Structure

1RO6 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Crystal structures of the catalytic domain of phosphodiesterase 4B complexed with AMP, 8-Br-AMP, and rolipram., Xu RX, Rocque WJ, Lambert MH, Vanderwall DE, Luther MA, Nolte RT, J Mol Biol. 2004 Mar 19;337(2):355-65. PMID:15003452 Page seeded by OCA on Sat May 3 07:43:12 2008

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