3frg

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{{Seed}}
 
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[[Image:3frg.jpg|left|200px]]
 
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==Catalytic Domain of Human Phosphodiesterase 4B2B in Complex with a Quinoline Inhibitor==
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The line below this paragraph, containing "STRUCTURE_3frg", creates the "Structure Box" on the page.
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<StructureSection load='3frg' size='340' side='right'caption='[[3frg]], [[Resolution|resolution]] 1.70&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'>[[3frg]] 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=3FRG OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3FRG 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]] 1.7&#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=ARS:ARSENIC'>ARS</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=SK4:4-[(3-METHOXYPHENYL)AMINO]-6-(METHYLSULFONYL)QUINOLINE-3-CARBOXAMIDE'>SK4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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{{STRUCTURE_3frg| PDB=3frg | 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=3frg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3frg OCA], [https://pdbe.org/3frg PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3frg RCSB], [https://www.ebi.ac.uk/pdbsum/3frg PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3frg ProSAT]</span></td></tr>
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</table>
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== Function ==
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[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/fr/3frg_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=3frg ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Crystallography-driven optimisation of a lead derived from similarity searching of the GSK compound collection resulted in the discovery of a series of quinoline derivatives that were highly potent and selective inhibitors of PDE4 with a good pharmacokinetic profile in the rat. Quinolines 43 and 48 have potential as oral medicines for the treatment of COPD.
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===Catalytic Domain of Human Phosphodiesterase 4B2B in Complex with a Quinoline Inhibitor===
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Quinolines as a novel structural class of potent and selective PDE4 inhibitors: optimisation for oral administration.,Lunniss CJ, Cooper AW, Eldred CD, Kranz M, Lindvall M, Lucas FS, Neu M, Preston AG, Ranshaw LE, Redgrave AJ, Ed Robinson J, Shipley TJ, Solanke YE, Somers DO, Wiseman JO Bioorg Med Chem Lett. 2009 Mar 1;19(5):1380-5. Epub 2009 Jan 19. PMID:19195882<ref>PMID:19195882</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 3frg" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_19195882}}, adds the Publication Abstract to the page
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*[[Phosphodiesterase 3D structures|Phosphodiesterase 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 19195882 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_19195882}}
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__TOC__
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</StructureSection>
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==About this Structure==
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3FRG is a 1 chain 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=3FRG OCA].
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==Reference==
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<ref group="xtra">PMID:19195882</ref><references group="xtra"/>
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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: Neu, M.]]
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[[Category: Large Structures]]
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[[Category: Somers, D O.]]
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[[Category: Neu M]]
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[[Category: Alternative splicing]]
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[[Category: Somers DO]]
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[[Category: Camp]]
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[[Category: Hydrolase]]
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[[Category: Hydrolase/hydrolase inhibitor complex]]
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[[Category: Pde]]
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[[Category: Phosphodiesterase]]
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[[Category: Phosphoprotein]]
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[[Category: Polymorphism]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 13 13:53:13 2010''
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Current revision

Catalytic Domain of Human Phosphodiesterase 4B2B in Complex with a Quinoline Inhibitor

PDB ID 3frg

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