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4c7k
From Proteopedia
(Difference between revisions)
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== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[4c7k]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4C7K OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4C7K FirstGlance]. <br> | <table><tr><td colspan='2'>[[4c7k]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4C7K OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4C7K FirstGlance]. <br> | ||
| - | </td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DZL:2-ETHYL-N-[(1S,3R)-5-OXIDANYL-2-ADAMANTYL]-4-[(2R)-OXOLAN-2-YL]-1,3-THIAZOLE-5-CARBOXAMIDE'>DZL</scene>, <scene name='pdbligand=NAP:NADP+NICOTINAMIDE-ADENINE-DINUCLEOTIDE+PHOSPHATE'>NAP</scene>< | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DZL:2-ETHYL-N-[(1S,3R)-5-OXIDANYL-2-ADAMANTYL]-4-[(2R)-OXOLAN-2-YL]-1,3-THIAZOLE-5-CARBOXAMIDE'>DZL</scene>, <scene name='pdbligand=NAP:NADP+NICOTINAMIDE-ADENINE-DINUCLEOTIDE+PHOSPHATE'>NAP</scene></td></tr> |
| - | <tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4c7j|4c7j]]</td></tr> | + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4c7j|4c7j]]</td></tr> |
| - | <tr><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='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><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4c7k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4c7k OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4c7k RCSB], [http://www.ebi.ac.uk/pdbsum/4c7k PDBsum]</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=4c7k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4c7k OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4c7k RCSB], [http://www.ebi.ac.uk/pdbsum/4c7k PDBsum]</span></td></tr> |
| - | <table> | + | </table> |
== Disease == | == Disease == | ||
[[http://www.uniprot.org/uniprot/DHI1_HUMAN DHI1_HUMAN]] Defects in HSD11B1 are a cause of cortisone reductase deficiency (CRD) [MIM:[http://omim.org/entry/604931 604931]]. In CRD, activation of cortisone to cortisol does not occur, resulting in adrenocorticotropin-mediated androgen excess and a phenotype resembling polycystic ovary syndrome (PCOS). | [[http://www.uniprot.org/uniprot/DHI1_HUMAN DHI1_HUMAN]] Defects in HSD11B1 are a cause of cortisone reductase deficiency (CRD) [MIM:[http://omim.org/entry/604931 604931]]. In CRD, activation of cortisone to cortisol does not occur, resulting in adrenocorticotropin-mediated androgen excess and a phenotype resembling polycystic ovary syndrome (PCOS). | ||
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Optimization of brain penetrant 11beta-hydroxysteroid dehydrogenase type I inhibitors and in vivo testing in diet-induced obese mice.,Goldberg FW, Dossetter AG, Scott JS, Robb GR, Boyd S, Groombridge SD, Kemmitt PD, Sjogren T, Gutierrez PM, deSchoolmeester J, Swales JG, Turnbull AV, Wild MJ J Med Chem. 2014 Feb 13;57(3):970-86. doi: 10.1021/jm4016729. Epub 2014 Jan 27. PMID:24422550<ref>PMID:24422550</ref> | Optimization of brain penetrant 11beta-hydroxysteroid dehydrogenase type I inhibitors and in vivo testing in diet-induced obese mice.,Goldberg FW, Dossetter AG, Scott JS, Robb GR, Boyd S, Groombridge SD, Kemmitt PD, Sjogren T, Gutierrez PM, deSchoolmeester J, Swales JG, Turnbull AV, Wild MJ J Med Chem. 2014 Feb 13;57(3):970-86. doi: 10.1021/jm4016729. Epub 2014 Jan 27. PMID:24422550<ref>PMID:24422550</ref> | ||
| - | From | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> |
</div> | </div> | ||
== References == | == References == | ||
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[[Category: 11-beta-hydroxysteroid dehydrogenase]] | [[Category: 11-beta-hydroxysteroid dehydrogenase]] | ||
[[Category: Human]] | [[Category: Human]] | ||
| - | [[Category: Boyd, S | + | [[Category: Boyd, S]] |
| - | [[Category: Dossetter, A G | + | [[Category: Dossetter, A G]] |
| - | [[Category: Goldberg, F W | + | [[Category: Goldberg, F W]] |
| - | [[Category: Groombridge, S D | + | [[Category: Groombridge, S D]] |
| - | [[Category: Gutierrez, P Morentin | + | [[Category: Gutierrez, P Morentin]] |
| - | [[Category: Kemmitt, P D | + | [[Category: Kemmitt, P D]] |
| - | [[Category: Robb, G R | + | [[Category: Robb, G R]] |
| - | [[Category: Schoolmeester, J de | + | [[Category: Schoolmeester, J de]] |
| - | [[Category: Scott, J S | + | [[Category: Scott, J S]] |
| - | [[Category: Sjogren, T | + | [[Category: Sjogren, T]] |
| - | [[Category: Swales, J G | + | [[Category: Swales, J G]] |
| - | [[Category: Turnbull, A V | + | [[Category: Turnbull, A V]] |
| - | [[Category: Wild, M J | + | [[Category: Wild, M J]] |
[[Category: Cns penetration]] | [[Category: Cns penetration]] | ||
[[Category: Oxidoreductase]] | [[Category: Oxidoreductase]] | ||
[[Category: Structure-based design]] | [[Category: Structure-based design]] | ||
Revision as of 13:09, 4 January 2015
11b-Hydroxysteroid Dehydrogenase Type I in complex with inhibitor
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Categories: 11-beta-hydroxysteroid dehydrogenase | Human | Boyd, S | Dossetter, A G | Goldberg, F W | Groombridge, S D | Gutierrez, P Morentin | Kemmitt, P D | Robb, G R | Schoolmeester, J de | Scott, J S | Sjogren, T | Swales, J G | Turnbull, A V | Wild, M J | Cns penetration | Oxidoreductase | Structure-based design
