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1xoz

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[[Image:1xoz.gif|left|200px]]
 
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{{Structure
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==Catalytic Domain Of Human Phosphodiesterase 5A In Complex With Tadalafil==
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|PDB= 1xoz |SIZE=350|CAPTION= <scene name='initialview01'>1xoz</scene>, resolution 1.37&Aring;
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<StructureSection load='1xoz' size='340' side='right'caption='[[1xoz]], [[Resolution|resolution]] 1.37&Aring;' scene=''>
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|SITE=
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== Structural highlights ==
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|LIGAND= <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene> and <scene name='pdbligand=CIA:6-BENZO[1,3]DIOXOL-5-YL-2-METHYL-2,3,6,7,12,12A-HEXAHYDRO-PYRAZINO[1',2':1,6]PYRIDO[3,4-B]INDOLE-1,4-DIONE'>CIA</scene>
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<table><tr><td colspan='2'>[[1xoz]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1XOZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1XOZ FirstGlance]. <br>
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|ACTIVITY= [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]
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.37&#8491;</td></tr>
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|GENE= PDE5A, PDE5 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CIA:6-BENZO[1,3]DIOXOL-5-YL-2-METHYL-2,3,6,7,12,12A-HEXAHYDRO-PYRAZINO[1,2 1,6]PYRIDO[3,4-B]INDOLE-1,4-DIONE'>CIA</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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}}
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1xoz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1xoz OCA], [https://pdbe.org/1xoz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1xoz RCSB], [https://www.ebi.ac.uk/pdbsum/1xoz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1xoz ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/PDE5A_HUMAN PDE5A_HUMAN] Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP.
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/xo/1xoz_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1xoz ConSurf].
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<div style="clear:both"></div>
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'''Catalytic Domain Of Human Phosphodiesterase 5A In Complex With Tadalafil'''
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==See Also==
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*[[Phosphodiesterase 3D structures|Phosphodiesterase 3D structures]]
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__TOC__
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==Overview==
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</StructureSection>
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Phosphodiesterases (PDEs) comprise a large family of enzymes that catalyze the hydrolysis of cAMP or cGMP and are implicated in various diseases. We describe the high-resolution crystal structures of the catalytic domains of PDE4B, PDE4D, and PDE5A with ten different inhibitors, including the drug candidates cilomilast and roflumilast, for respiratory diseases. These cocrystal structures reveal a common scheme of inhibitor binding to the PDEs: (i) a hydrophobic clamp formed by highly conserved hydrophobic residues that sandwich the inhibitor in the active site; (ii) hydrogen bonding to an invariant glutamine that controls the orientation of inhibitor binding. A scaffold can be readily identified for any given inhibitor based on the formation of these two types of conserved interactions. These structural insights will enable the design of isoform-selective inhibitors with improved binding affinity and should facilitate the discovery of more potent and selective PDE inhibitors for the treatment of a variety of diseases.
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==About this Structure==
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1XOZ is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1XOZ OCA].
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==Reference==
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Structural basis for the activity of drugs that inhibit phosphodiesterases., Card GL, England BP, Suzuki Y, Fong D, Powell B, Lee B, Luu C, Tabrizizad M, Gillette S, Ibrahim PN, Artis DR, Bollag G, Milburn MV, Kim SH, Schlessinger J, Zhang KY, Structure. 2004 Dec;12(12):2233-47. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15576036 15576036]
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[[Category: 3',5'-cyclic-nucleotide phosphodiesterase]]
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Single protein]]
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[[Category: Large Structures]]
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[[Category: Artis, D R.]]
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[[Category: Artis DR]]
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[[Category: Bollag, G.]]
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[[Category: Bollag G]]
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[[Category: Card, G L.]]
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[[Category: Card GL]]
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[[Category: England, B P.]]
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[[Category: England BP]]
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[[Category: Fong, D.]]
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[[Category: Fong D]]
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[[Category: Gillette, S.]]
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[[Category: Gillette S]]
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[[Category: Ibrahim, P N.]]
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[[Category: Ibrahim PN]]
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[[Category: Kim, S H.]]
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[[Category: Kim S-H]]
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[[Category: Lee, B.]]
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[[Category: Lee B]]
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[[Category: Luu, C.]]
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[[Category: Luu C]]
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[[Category: Milburn, M V.]]
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[[Category: Milburn MV]]
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[[Category: Powell, B.]]
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[[Category: Powell B]]
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[[Category: Schlessinger, J.]]
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[[Category: Schlessinger J]]
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[[Category: Suzuki, Y.]]
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[[Category: Suzuki Y]]
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[[Category: Tabrizizad, M.]]
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[[Category: Tabrizizad M]]
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[[Category: Zhang, K Y.J.]]
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[[Category: Zhang KYJ]]
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[[Category: CIA]]
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[[Category: MG]]
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[[Category: ZN]]
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[[Category: ciali]]
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[[Category: pde]]
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[[Category: pde5a]]
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[[Category: phosphodiesterase]]
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[[Category: tadalafil]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 15:12:41 2008''
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Current revision

Catalytic Domain Of Human Phosphodiesterase 5A In Complex With Tadalafil

PDB ID 1xoz

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