2ilt | pdb_00002ilt
Human 11-beta-Hydroxysteroid Dehydrogenase (HSD1) with NADP and Adamantane Sulfone Inhibitor
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| 2ilt, resolution 2.300Å | |||||||||||||
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| Ligands: | NI, NAP and NN1 | ||||||||||||
| Gene: | HSD11B1 (Homo sapiens) | ||||||||||||
| Activity: | 11-beta-hydroxysteroid dehydrogenase, with EC number 1.1.1.146 | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
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
