3lz6

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==Guinea Pig 11beta hydroxysteroid dehydrogenase with PF-877423==
==Guinea Pig 11beta hydroxysteroid dehydrogenase with PF-877423==
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<StructureSection load='3lz6' size='340' side='right' caption='[[3lz6]], [[Resolution|resolution]] 1.84&Aring;' scene=''>
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<StructureSection load='3lz6' size='340' side='right'caption='[[3lz6]], [[Resolution|resolution]] 1.84&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[3lz6]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Cavia_porcellus Cavia porcellus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3LZ6 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3LZ6 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[3lz6]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Cavia_porcellus Cavia porcellus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3LZ6 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3LZ6 FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=A0D:N-ADAMANTAN-2-YL-1-ETHYL-D-PROLINAMIDE'>A0D</scene>, <scene name='pdbligand=NAP:NADP+NICOTINAMIDE-ADENINE-DINUCLEOTIDE+PHOSPHATE'>NAP</scene></td></tr>
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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]] 1.84&#8491;</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">HSD11B1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10141 Cavia porcellus])</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=A0D:N-ADAMANTAN-2-YL-1-ETHYL-D-PROLINAMIDE'>A0D</scene>, <scene name='pdbligand=NAP:NADP+NICOTINAMIDE-ADENINE-DINUCLEOTIDE+PHOSPHATE'>NAP</scene></td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/11-beta-hydroxysteroid_dehydrogenase 11-beta-hydroxysteroid dehydrogenase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.1.1.146 1.1.1.146] </span></td></tr>
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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=3lz6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3lz6 OCA], [https://pdbe.org/3lz6 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3lz6 RCSB], [https://www.ebi.ac.uk/pdbsum/3lz6 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3lz6 ProSAT]</span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3lz6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3lz6 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3lz6 RCSB], [http://www.ebi.ac.uk/pdbsum/3lz6 PDBsum]</span></td></tr>
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</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/DHI1_CAVPO DHI1_CAVPO]] Catalyzes reversibly the conversion of cortisol to the inactive metabolite cortisone. Catalyzes reversibly the conversion of 7-ketocholesterol to 7-beta-hydroxycholesterol. In intact cells, the reaction runs only in one direction, from 7-ketocholesterol to 7-beta-hydroxycholesterol (By similarity).<ref>PMID:10699594</ref>
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[https://www.uniprot.org/uniprot/DHI1_CAVPO DHI1_CAVPO] Catalyzes reversibly the conversion of cortisol to the inactive metabolite cortisone. Catalyzes reversibly the conversion of 7-ketocholesterol to 7-beta-hydroxycholesterol. In intact cells, the reaction runs only in one direction, from 7-ketocholesterol to 7-beta-hydroxycholesterol (By similarity).<ref>PMID:10699594</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The design and development of a series of highly selective pyrrolidine carboxamide 11beta-HSD1 inhibitors are described. These compounds including PF-877423 demonstrated potent in vitro activity against both human and mouse 11beta-HSD1 enzymes. In an in vivo assay, PF-877423 inhibited the conversion of cortisone to cortisol. Structure guided optimization effort yielded potent and stable 11beta-HSD1 selective inhibitor 42.
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The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors.,Cheng H, Hoffman J, Le P, Nair SK, Cripps S, Matthews J, Smith C, Yang M, Kupchinsky S, Dress K, Edwards M, Cole B, Walters E, Loh C, Ermolieff J, Fanjul A, Bhat GB, Herrera J, Pauly T, Hosea N, Paderes G, Rejto P Bioorg Med Chem Lett. 2010 May 1;20(9):2897-902. Epub 2010 Mar 10. PMID:20363126<ref>PMID:20363126</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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==See Also==
==See Also==
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*[[Hydroxysteroid dehydrogenase|Hydroxysteroid dehydrogenase]]
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*[[Hydroxysteroid dehydrogenase 3D structures|Hydroxysteroid dehydrogenase 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: 11-beta-hydroxysteroid dehydrogenase]]
 
[[Category: Cavia porcellus]]
[[Category: Cavia porcellus]]
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[[Category: Pauly, T A]]
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[[Category: Large Structures]]
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[[Category: Oxidoreductase-oxidoreductase inhibitor complex]]
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[[Category: Pauly TA]]

Current revision

Guinea Pig 11beta hydroxysteroid dehydrogenase with PF-877423

PDB ID 3lz6

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