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6F5H

Crystal structure of USP7 in complex with a 4-hydroxypiperidine based inhibitor

6F5H の概要
エントリーDOI10.2210/pdb6f5h/pdb
関連するPDBエントリー5N9R 5N9T
分子名称Ubiquitin carboxyl-terminal hydrolase 7, SULFATE ION, GLYCEROL, ... (5 entities in total)
機能のキーワードusp7, reversible, inhibitor, selective, hydrolase
由来する生物種Homo sapiens (Human)
細胞内の位置Nucleus : Q93009
タンパク質・核酸の鎖数2
化学式量合計84327.20
構造登録者
主引用文献O'Dowd, C.R.,Helm, M.D.,Rountree, J.S.S.,Flasz, J.T.,Arkoudis, E.,Miel, H.,Hewitt, P.R.,Jordan, L.,Barker, O.,Hughes, C.,Rozycka, E.,Cassidy, E.,McClelland, K.,Odrzywol, E.,Page, N.,Feutren-Burton, S.,Dvorkin, S.,Gavory, G.,Harrison, T.
Identification and Structure-Guided Development of Pyrimidinone Based USP7 Inhibitors.
ACS Med Chem Lett, 9:238-243, 2018
Cited by
PubMed Abstract: Ubiquitin specific protease 7 (USP7, HAUSP) has become an attractive target in drug discovery due to the role it plays in modulating Mdm2 levels and consequently p53. Increasing interest in USP7 is emerging due to its potential involvement in oncogenic pathways as well as possible roles in both metabolic and immune disorders in addition to viral infections. Potent, novel, and selective inhibitors of USP7 have been developed using both rational and structure-guided design enabled by high-resolution cocrystallography. Initial hits were identified via fragment-based screening, scaffold-hopping, and hybridization exercises. Two distinct subseries are described along with associated structure-activity relationship trends, as are initial efforts aimed at developing compounds suitable for experiments. Overall, these discoveries will enable further research into the wider biological role of USP7.
PubMed: 29541367
DOI: 10.1021/acsmedchemlett.7b00512
主引用文献が同じPDBエントリー
実験手法
X-RAY DIFFRACTION (2.16 Å)
構造検証レポート
Validation report summary of 6f5h
検証レポート(詳細版)ダウンロードをダウンロード

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件を2025-10-22に公開中

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