2ilt
From Proteopedia
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|PDB= 2ilt |SIZE=350|CAPTION= <scene name='initialview01'>2ilt</scene>, resolution 2.300Å | |PDB= 2ilt |SIZE=350|CAPTION= <scene name='initialview01'>2ilt</scene>, resolution 2.300Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= <scene name='pdbligand= | + | |LIGAND= <scene name='pdbligand=NAP:NADP+NICOTINAMIDE-ADENINE-DINUCLEOTIDE+PHOSPHATE'>NAP</scene>, <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</scene>, <scene name='pdbligand=NN1:2-(2-CHLORO-4-FLUOROPHENOXY)-2-METHYL-N-[(1R,2S,3S,5S,7S)-5-(METHYLSULFONYL)-2-ADAMANTYL]PROPANAMIDE'>NN1</scene> |
| - | |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] | + | |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> |
|GENE= HSD11B1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= HSD11B1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2ilt FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ilt OCA], [http://www.ebi.ac.uk/pdbsum/2ilt PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2ilt RCSB]</span> | ||
}} | }} | ||
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==Disease== | ==Disease== | ||
| - | Known | + | Known disease associated with this structure: Cortisone reductase deficiency OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=600713 600713]] |
==About this Structure== | ==About this Structure== | ||
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[[Category: Qin, W.]] | [[Category: Qin, W.]] | ||
[[Category: Sorensen, B.]] | [[Category: Sorensen, B.]] | ||
| - | [[Category: NAP]] | ||
| - | [[Category: NI]] | ||
| - | [[Category: NN1]] | ||
[[Category: hsd1]] | [[Category: hsd1]] | ||
[[Category: inhibitor]] | [[Category: inhibitor]] | ||
[[Category: nadp]] | [[Category: nadp]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:45:48 2008'' |
Revision as of 00:45, 31 March 2008
| |||||||
| , resolution 2.300Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , , | ||||||
| Gene: | HSD11B1 (Homo sapiens) | ||||||
| Activity: | 11-beta-hydroxysteroid dehydrogenase, with EC number 1.1.1.146 | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| 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 disease 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 Mon Mar 31 03:45:48 2008
