2ILT

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

2ILT の概要

• エントリーDOI: 10.2210/pdb2ilt/pdb
• 分子名称: Corticosteroid 11-beta-dehydrogenase isozyme 1, NICKEL (II) ION, NADP NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE, ... (5 entities in total)
• 機能のキーワード: hsd1, nadp, inhibitor, oxidoreductase
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Endoplasmic reticulum membrane ; Single-pass type II membrane protein : P28845
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 31722.86

構造登録者

Longenecker, K.L.,Sorensen, B.,Judge, R.,Qin, W.,Link, J.T. (登録日: 2006-10-03, 公開日: 2007-04-03, 最終更新日: 2024-02-21)

主引用文献

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, E.U.,Jacobson, P.,Link, J.T.
Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors.
Bioorg.Med.Chem.Lett., 17:527-532, 2007

PubMed Abstract: 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.

PubMed: 17070044
DOI: 10.1016/j.bmcl.2006.10.008

実験手法

X-RAY DIFFRACTION (2.3 Å)