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6WV6

Human VKOR with phenindione

6WV6 の概要
エントリーDOI10.2210/pdb6wv6/pdb
分子名称Vitamin K epoxide reductase, termini restrained by green fluorescent protein, (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, Phenindione, ... (4 entities in total)
機能のキーワードvitamin k epoxide reductase (vkor), vitamin k, warfarin, superwarfarin, phenindione, vitamin k expoxide(ko), membrane protein, oxidoreductase, fluorescent protein
由来する生物種Aequorea victoria (Jellyfish)
詳細
タンパク質・核酸の鎖数1
化学式量合計45132.75
構造登録者
Liu, S.,Sukumar, N.,Li, W. (登録日: 2020-05-05, 公開日: 2020-11-11, 最終更新日: 2024-11-06)
主引用文献Liu, S.,Li, S.,Shen, G.,Sukumar, N.,Krezel, A.M.,Li, W.
Structural basis of antagonizing the vitamin K catalytic cycle for anticoagulation.
Science, 371:-, 2021
Cited by
PubMed Abstract: Vitamin K antagonists are widely used anticoagulants that target vitamin K epoxide reductases (VKOR), a family of integral membrane enzymes. To elucidate their catalytic cycle and inhibitory mechanism, we report 11 x-ray crystal structures of human VKOR and pufferfish VKOR-like, with substrates and antagonists in different redox states. Substrates entering the active site in a partially oxidized state form cysteine adducts that induce an open-to-closed conformational change, triggering reduction. Binding and catalysis are facilitated by hydrogen-bonding interactions in a hydrophobic pocket. The antagonists bind specifically to the same hydrogen-bonding residues and induce a similar closed conformation. Thus, vitamin K antagonists act through mimicking the key interactions and conformational changes required for the VKOR catalytic cycle.
PubMed: 33154105
DOI: 10.1126/science.abc5667
主引用文献が同じPDBエントリー
実験手法
X-RAY DIFFRACTION (2.7 Å)
構造検証レポート
Validation report summary of 6wv6
検証レポート(詳細版)ダウンロードをダウンロード

227561

件を2024-11-20に公開中

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