6E37

O-GlcNAc Transferase in complex with covalent inhibitor

6E37 の概要

• エントリーDOI: 10.2210/pdb6e37/pdb
• 分子名称: O-GlcNAc transferase subunit p110, TYR-PRO-GLY-GLY-SER-THR-PRO-VAL-SER-SER-ALA-ASN, (2S,3R,4R,5S,6R)-3-[(2E)-but-2-enoylamino]-4,5-dihydroxy-6-(hydroxymethyl)tetrahydro-2H-thiopyran-2-yl [(2R,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-3,4-dihydroxytetrahydrofuran-2-yl]methyl dihydrogen diphosphate (non-preferred name), ... (4 entities in total)
• 機能のキーワード: o-glcnac transferase, inhibitor, transferase-inhibitor complex, transferase/inhibitor
• 由来する生物種: Homo sapiens (Human); 詳細
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 83022.53

構造登録者

Li, H.,Jiang, J. (登録日: 2018-07-13, 公開日: 2019-11-06, 最終更新日: 2024-10-16)

主引用文献

Worth, M.,Hu, C.W.,Li, H.,Fan, D.,Estevez, A.,Zhu, D.,Wang, A.,Jiang, J.
Targeted covalent inhibition of O-GlcNAc transferase in cells.
Chem.Commun.(Camb.), 55:13291-13294, 2019

PubMed Abstract: O-GlcNAc transferase (OGT) glycosylates numerous proteins and is implicated in many diseases. To date, most OGT inhibitors lack either sufficient potency or characterized specificity in cells. We report the first targeted covalent inhibitor that predominantly reacts with OGT but does not affect other functionally similar enzymes. This study provides a new strategy to interrogate cellular OGT functions and to investigate other glycosyltransferases.

PubMed: 31626249
DOI: 10.1039/c9cc04560k

実験手法

X-RAY DIFFRACTION (2.531 Å)