3OUJ

PHD2 with 2-Oxoglutarate

3OUJ の概要

• エントリーDOI: 10.2210/pdb3ouj/pdb
• 関連するPDBエントリー: 3OUH 3OUI
• 分子名称: Egl nine homolog 1, SULFATE ION, FE (II) ION, ... (5 entities in total)
• 機能のキーワード: phd2, 2og, oxidoreductase
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cytoplasm : Q9GZT9
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 26877.28

構造登録者

Staker, B.L.,Arakaki, T.L. (登録日: 2010-09-14, 公開日: 2010-12-01, 最終更新日: 2024-02-21)

主引用文献

Rosen, M.D.,Venkatesan, H.,Peltier, H.M.,Bembenek, S.D.,Kanelakis, K.C.,Zhao, L.X.,Leonard, B.E.,Hocutt, F.M.,Wu, X.,Palomino, H.L.,Brondstetter, T.I.,Haugh, P.V.,Cagnon, L.,Yan, W.,Liotta, L.A.,Young, A.,Mirzadegan, T.,Shankley, N.P.,Barrett, T.D.,Rabinowitz, M.H.
Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues.
ACS Med Chem Lett, 1:526-529, 2010

PubMed Abstract: HIF prolyl 4-hydroxylases (PHD) are a family of enzymes that mediate key physiological responses to hypoxia by modulating the levels of hypoxia inducible factor 1-α (HIF1α). Certain benzimidazole-2-pyrazole carboxylates were discovered to be PHD2 inhibitors using ligand- and structure-based methods and found to be potent, orally efficacious stimulators of erythropoietin secretion in vivo.

PubMed: 24900242
DOI: 10.1021/ml100198y

実験手法

X-RAY DIFFRACTION (2.3 Å)