3VN9

Rifined Crystal structure of non-phosphorylated MAP2K6 in a putative auto-inhibition state

「3AN0」から置き換えられました

3VN9 の概要

• エントリーDOI: 10.2210/pdb3vn9/pdb
• 分子名称: Dual specificity mitogen-activated protein kinase kinase 6, 9-{5-O-[(R)-hydroxy{[(S)-hydroxy(phosphonoamino)phosphoryl]oxy}phosphoryl]-beta-L-ribofuranosyl}-9H-purin-6-amine, MAGNESIUM ION, ... (4 entities in total)
• 機能のキーワード: auto-inhibition state, activation helices, mitogen-activated protein kinase kinase, amp-pnp binding, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Nucleus : P52564
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 38899.70

構造登録者

Kinoshita, T.,Matsuzaka, H.,Nakai, R.,Kirii, Y.,Yokota, K.,Tada, T.,Matsumoto, T. (登録日: 2012-01-05, 公開日: 2012-02-29, 最終更新日: 2023-11-08)

主引用文献

Matsumoto, T.,Kinoshita, T.,Matsuzaka, H.,Nakai, R.,Kirii, Y.,Yokota, K.,Tada, T.
Crystal structure of non-phosphorylated MAP2K6 in a putative auto-inhibition state
J.Biochem., 151:541-549, 2012

PubMed Abstract: Mitogen-activated protein kinase kinase 6 (MAP2K6) plays a crucial role in the p38 MAP kinase signal cascade that regulates various stress-induced responses and is associated with pathological conditions. The crystal structure of human non-phosphorylated MAP2K6 (npMAP2K6) complexed with an ATP analogue was determined at 2.6 Å resolution and represents an auto-inhibition state of MAP2K6. Three characteristics of short α-helices configured in the activation loop region, termed activation helices (AH1, AH2 and AH3), are important in controlling the auto-inhibition mechanism. AH1 displaces the αC-helix, a component essential for forming the active configuration, away from the active site. AH1 and AH2 were found to enclose the γ-phosphate, the leaving group of ATP. A comparison with the related enzymes, MAP2K1 and MAP2K4 reveals that MAP2K6 has the unique auto-inhibition mechanism mediated by the three activation helices.

PubMed: 22383536
DOI: 10.1093/jb/mvs023

実験手法

X-RAY DIFFRACTION (2.6 Å)