2chm: Difference between revisions

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{{Seed}}
[[Image:2chm.png|left|200px]]


<!--
==Crystal structure of N2 substituted pyrazolo pyrimidinones - a flipped binding mode in PDE5==
The line below this paragraph, containing "STRUCTURE_2chm", creates the "Structure Box" on the page.
<StructureSection load='2chm' size='340' side='right'caption='[[2chm]], [[Resolution|resolution]] 1.60&Aring;' scene=''>
You may change the PDB parameter (which sets the PDB file loaded into the applet)  
== Structural highlights ==
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
<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>
or leave the SCENE parameter empty for the default display.
</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>
-->
<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>
{{STRUCTURE_2chm| PDB=2chm |  SCENE= }}
<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>
</table>
== Function ==
[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>
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
Check<jmol>
  <jmolCheckbox>
    <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/ch/2chm_consurf.spt"</scriptWhenChecked>
    <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
    <text>to colour the structure by Evolutionary Conservation</text>
  </jmolCheckbox>
</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].
<div style="clear:both"></div>


===CRYSTAL STRUCTURE OF N2 SUBSTITUTED PYRAZOLO PYRIMIDINONES-A FLIPPED BINDING MODE IN PDE5===
==See Also==
 
*[[Phosphodiesterase 3D structures|Phosphodiesterase 3D structures]]
 
== References ==
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<references/>
The line below this paragraph, {{ABSTRACT_PUBMED_16759100}}, adds the Publication Abstract to the page
__TOC__
(as it appears on PubMed at http://www.pubmed.gov), where 16759100 is the PubMed ID number.
</StructureSection>
-->
{{ABSTRACT_PUBMED_16759100}}
 
==About this Structure==
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].
 
==Reference==
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]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Large Structures]]
[[Category: Allerton, C M.N.]]
[[Category: Allerton CMN]]
[[Category: Barber, C G.]]
[[Category: Barber CG]]
[[Category: Beaumont, K C.]]
[[Category: Beaumont KC]]
[[Category: Brown, D G.]]
[[Category: Brown DG]]
[[Category: Cole, S M.]]
[[Category: Cole SM]]
[[Category: Ellis, D.]]
[[Category: Ellis D]]
[[Category: Lane, C A.L.]]
[[Category: Lane CAL]]
[[Category: Maw, G N.]]
[[Category: Maw GN]]
[[Category: Mount, N M.]]
[[Category: Mount NM]]
[[Category: Rawson, D J.]]
[[Category: Rawson DJ]]
[[Category: Robinson, C M.]]
[[Category: Robinson CM]]
[[Category: Street, S D.A.]]
[[Category: Street SDA]]
[[Category: Summerhill, N W.]]
[[Category: Summerhill NW]]
[[Category: Allosteric enzyme]]
[[Category: Alternative splicing]]
[[Category: Camp]]
[[Category: Cgmp]]
[[Category: Cgmp-binding]]
[[Category: Chimera]]
[[Category: Hydrolase]]
[[Category: Inhibitor]]
[[Category: Magnesium]]
[[Category: Metal-binding]]
[[Category: Nucleotide-binding]]
[[Category: Phosphodiesterase 5]]
[[Category: Phosphorylation]]
[[Category: Zinc]]
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 12:21:54 2008''
Retrieved from "https://proteopedia.org/2chm"