2ilt

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Image:2ilt.jpg

2ilt, resolution 2.300Å

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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 with , and as ligands. Active as 11-beta-hydroxysteroid dehydrogenase, with EC number 1.1.1.146 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

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