2irw

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[[Image:2irw.gif|left|200px]]
[[Image:2irw.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2irw |SIZE=350|CAPTION= <scene name='initialview01'>2irw</scene>, resolution 3.100&Aring;
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The line below this paragraph, containing "STRUCTURE_2irw", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=NAP:NADP+NICOTINAMIDE-ADENINE-DINUCLEOTIDE+PHOSPHATE'>NAP</scene>, <scene name='pdbligand=NN4:(1S,3R,4S,5S,7S)-4-{[2-(4-METHOXYPHENOXY)-2-METHYLPROPANOYL]AMINO}ADAMANTANE-1-CARBOXAMIDE'>NN4</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <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>
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or leave the SCENE parameter empty for the default display.
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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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|DOMAIN=
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{{STRUCTURE_2irw| PDB=2irw | SCENE= }}
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|RELATEDENTRY=[[2ilt|2ILT]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2irw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2irw OCA], [http://www.ebi.ac.uk/pdbsum/2irw PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2irw RCSB]</span>
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}}
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'''Human 11-beta-Hydroxysteroid Dehydrogenase (HSD1) with NADP and Adamantane Ether Inhibitor'''
'''Human 11-beta-Hydroxysteroid Dehydrogenase (HSD1) with NADP and Adamantane Ether Inhibitor'''
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[[Category: Qin, W.]]
[[Category: Qin, W.]]
[[Category: Russell, J.]]
[[Category: Russell, J.]]
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[[Category: hsd1]]
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[[Category: Hsd1]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: nadp]]
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[[Category: Nadp]]
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[[Category: oxidoreductase]]
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[[Category: Oxidoreductase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 07:47:35 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:47:39 2008''
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Revision as of 04:47, 4 May 2008

Image:2irw.gif

Template:STRUCTURE 2irw

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


Contents

Overview

A novel class of adamantane ethers 11beta-hydroxysteroid hydrogenase type I inhibitors has been discovered. These compounds have excellent HSD-1 potency and selectivity against HSD-2. The structure-activity relationships, selectivity, metabolism, PK, ex vivo pharmacodynamic data, and an X-ray crystal structure of one of these inhibitors bound to h-HSD-1 are discussed.

Disease

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

About this Structure

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

Reference

Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation., Patel JR, Shuai Q, Dinges J, Winn M, Pliushchev M, Fung S, Monzon K, Chiou W, Wang J, Pan L, Wagaw S, Engstrom K, Kerdesky FA, Longenecker K, Judge R, Qin W, Imade HM, Stolarik D, Beno DW, Brune M, Chovan LE, Sham HL, Jacobson P, Link JT, Bioorg Med Chem Lett. 2007 Feb 1;17(3):750-5. Epub 2006 Oct 28. PMID:17110106 Page seeded by OCA on Sun May 4 07:47:35 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

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