3lz6
From Proteopedia
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| - | [[ | + | ==Guinea Pig 11beta hydroxysteroid dehydrogenase with PF-877423== |
| + | <StructureSection load='3lz6' size='340' side='right' caption='[[3lz6]], [[Resolution|resolution]] 1.84Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <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> | ||
| + | </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> | ||
| + | <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> | ||
| + | <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> | ||
| + | <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> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | 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. | ||
| - | + | 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> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
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==See Also== | ==See Also== | ||
*[[Hydroxysteroid dehydrogenase|Hydroxysteroid dehydrogenase]] | *[[Hydroxysteroid dehydrogenase|Hydroxysteroid dehydrogenase]] | ||
| - | + | == References == | |
| - | == | + | <references/> |
| - | < | + | __TOC__ |
| + | </StructureSection> | ||
[[Category: 11-beta-hydroxysteroid dehydrogenase]] | [[Category: 11-beta-hydroxysteroid dehydrogenase]] | ||
[[Category: Cavia porcellus]] | [[Category: Cavia porcellus]] | ||
| - | [[Category: Pauly, T A | + | [[Category: Pauly, T A]] |
[[Category: Oxidoreductase-oxidoreductase inhibitor complex]] | [[Category: Oxidoreductase-oxidoreductase inhibitor complex]] | ||
Revision as of 09:44, 9 December 2014
Guinea Pig 11beta hydroxysteroid dehydrogenase with PF-877423
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