2chm

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{{Seed}}
 
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[[Image:2chm.png|left|200px]]
 
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==Crystal structure of N2 substituted pyrazolo pyrimidinones - a flipped binding mode in PDE5==
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The line below this paragraph, containing "STRUCTURE_2chm", creates the "Structure Box" on the page.
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<StructureSection load='2chm' size='340' side='right'caption='[[2chm]], [[Resolution|resolution]] 1.60&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[2chm]] 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=2CHM OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2CHM FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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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]] 1.6&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=3P4:5-[2-(BUT-3-EN-1-YLOXY)-5-(1-HYDROXYVINYL)PYRIDIN-3-YL]-3-ETHYL-2-(1-ETHYLAZETIDIN-3-YL)-1,2,6,7A-TETRAHYDRO-7H-PYRAZOLO[4,3-D]PYRIMIDIN-7-ONE'>3P4</scene>, <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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{{STRUCTURE_2chm| PDB=2chm | SCENE= }}
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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=2chm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2chm OCA], [https://pdbe.org/2chm PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2chm RCSB], [https://www.ebi.ac.uk/pdbsum/2chm PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2chm 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.[https://www.uniprot.org/uniprot/PDE4B_HUMAN PDE4B_HUMAN] Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. May be involved in mediating central nervous system effects of therapeutic agents ranging from antidepressants to antiasthmatic and anti-inflammatory agents.<ref>PMID:10846163</ref> <ref>PMID:15003452</ref>
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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/ch/2chm_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=2chm ConSurf].
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<div style="clear:both"></div>
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===CRYSTAL STRUCTURE OF N2 SUBSTITUTED PYRAZOLO PYRIMIDINONES-A FLIPPED BINDING MODE IN PDE5===
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==See Also==
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*[[Phosphodiesterase 3D structures|Phosphodiesterase 3D structures]]
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== References ==
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<references/>
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The line below this paragraph, {{ABSTRACT_PUBMED_16759100}}, adds the Publication Abstract to the page
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__TOC__
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(as it appears on PubMed at http://www.pubmed.gov), where 16759100 is the PubMed ID number.
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</StructureSection>
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{{ABSTRACT_PUBMED_16759100}}
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==About this Structure==
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2CHM 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=2CHM OCA].
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==Reference==
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A novel series of potent and selective PDE5 inhibitors with potential for high and dose-independent oral bioavailability., Allerton CM, Barber CG, Beaumont KC, Brown DG, Cole SM, Ellis D, Lane CA, Maw GN, Mount NM, Rawson DJ, Robinson CM, Street SD, Summerhill NW, J Med Chem. 2006 Jun 15;49(12):3581-94. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16759100 16759100]
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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: Allerton, C M.N.]]
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[[Category: Allerton CMN]]
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[[Category: Barber, C G.]]
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[[Category: Barber CG]]
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[[Category: Beaumont, K C.]]
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[[Category: Beaumont KC]]
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[[Category: Brown, D G.]]
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[[Category: Brown DG]]
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[[Category: Cole, S M.]]
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[[Category: Cole SM]]
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[[Category: Ellis, D.]]
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[[Category: Ellis D]]
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[[Category: Lane, C A.L.]]
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[[Category: Lane CAL]]
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[[Category: Maw, G N.]]
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[[Category: Maw GN]]
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[[Category: Mount, N M.]]
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[[Category: Mount NM]]
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[[Category: Rawson, D J.]]
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[[Category: Rawson DJ]]
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[[Category: Robinson, C M.]]
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[[Category: Robinson CM]]
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[[Category: Street, S D.A.]]
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[[Category: Street SDA]]
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[[Category: Summerhill, N W.]]
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[[Category: Summerhill NW]]
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[[Category: Allosteric enzyme]]
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[[Category: Alternative splicing]]
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[[Category: Camp]]
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[[Category: Cgmp]]
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[[Category: Cgmp-binding]]
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[[Category: Chimera]]
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[[Category: Hydrolase]]
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[[Category: Inhibitor]]
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[[Category: Magnesium]]
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[[Category: Metal-binding]]
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[[Category: Nucleotide-binding]]
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[[Category: Phosphodiesterase 5]]
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[[Category: Phosphorylation]]
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[[Category: Zinc]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 12:21:54 2008''
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Current revision

Crystal structure of N2 substituted pyrazolo pyrimidinones - a flipped binding mode in PDE5

PDB ID 2chm

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