2ilt

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[[Image:2ilt.jpg|left|200px]]<br /><applet load="2ilt" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2ilt.jpg|left|200px]]
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caption="2ilt, resolution 2.300&Aring;" />
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'''Human 11-beta-Hydroxysteroid Dehydrogenase (HSD1) with NADP and Adamantane Sulfone Inhibitor'''<br />
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{{Structure
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|PDB= 2ilt |SIZE=350|CAPTION= <scene name='initialview01'>2ilt</scene>, resolution 2.300&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</scene>, <scene name='pdbligand=NAP:NADP+NICOTINAMIDE-ADENINE-DINUCLEOTIDE+PHOSPHATE'>NAP</scene> and <scene name='pdbligand=NN1:2-(2-CHLORO-4-FLUOROPHENOXY)-2-METHYL-N-[(1R,2S,3S,5S,7S)-5-(METHYLSULFONYL)-2-ADAMANTYL]PROPANAMIDE'>NN1</scene>
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|ACTIVITY= [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]
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|GENE= HSD11B1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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}}
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'''Human 11-beta-Hydroxysteroid Dehydrogenase (HSD1) with NADP and Adamantane Sulfone Inhibitor'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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2ILT is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=NI:'>NI</scene>, <scene name='pdbligand=NAP:'>NAP</scene> and <scene name='pdbligand=NN1:'>NN1</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2ILT OCA].
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2ILT 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=2ILT OCA].
==Reference==
==Reference==
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Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors., Sorensen B, Winn M, Rohde J, Shuai Q, Wang J, Fung S, Monzon K, Chiou W, Stolarik D, Imade H, Pan L, Deng X, Chovan L, Longenecker K, Judge R, Qin W, Brune M, Camp H, Frevert EU, Jacobson P, Link JT, Bioorg Med Chem Lett. 2007 Jan 15;17(2):527-32. Epub 2006 Oct 7. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17070044 17070044]
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Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors., Sorensen B, Winn M, Rohde J, Shuai Q, Wang J, Fung S, Monzon K, Chiou W, Stolarik D, Imade H, Pan L, Deng X, Chovan L, Longenecker K, Judge R, Qin W, Brune M, Camp H, Frevert EU, Jacobson P, Link JT, Bioorg Med Chem Lett. 2007 Jan 15;17(2):527-32. Epub 2006 Oct 7. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17070044 17070044]
[[Category: 11-beta-hydroxysteroid dehydrogenase]]
[[Category: 11-beta-hydroxysteroid dehydrogenase]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: nadp]]
[[Category: nadp]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:53:52 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 17:30:55 2008''

Revision as of 15:30, 20 March 2008

Image:2ilt.jpg


PDB ID 2ilt

Drag the structure with the mouse to rotate
, resolution 2.300Å
Ligands: , and
Gene: HSD11B1 (Homo sapiens)
Activity: 11-beta-hydroxysteroid dehydrogenase, with EC number 1.1.1.146
Coordinates: save as pdb, mmCIF, xml



Human 11-beta-Hydroxysteroid Dehydrogenase (HSD1) with NADP and Adamantane Sulfone Inhibitor


Contents

Overview

Potent and selective adamantane sulfone and sulfonamide inhibitors of 11-beta-HSD-1 have been discovered. Selected compounds from these series have robust pharmacokinetic profiles and strongly inhibit liver, fat, and brain HSD1 for extended periods after oral dosing.

Disease

Known diseases associated with this structure: Cortisone reductase deficiency OMIM:[600713]

About this Structure

2ILT is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors., Sorensen B, Winn M, Rohde J, Shuai Q, Wang J, Fung S, Monzon K, Chiou W, Stolarik D, Imade H, Pan L, Deng X, Chovan L, Longenecker K, Judge R, Qin W, Brune M, Camp H, Frevert EU, Jacobson P, Link JT, Bioorg Med Chem Lett. 2007 Jan 15;17(2):527-32. Epub 2006 Oct 7. PMID:17070044

Page seeded by OCA on Thu Mar 20 17:30:55 2008

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