2Y5K

Orally active aminopyridines as inhibitors of tetrameric fructose 1,6- bisphosphatase

2Y5K の概要

• エントリーDOI: 10.2210/pdb2y5k/pdb
• 関連するPDBエントリー: 1FTA 2FHY 2FIE 2FIX 2JJK 2VT5 2WBB 2WBD 2Y5L
• 分子名称: FRUCTOSE-1,6-BISPHOSPHATASE 1, 1-[5-(2-METHOXYETHYL)-4-METHYL-THIOPHEN-2-YL]SULFONYL-3-[4-METHOXY-6-(METHYLCARBAMOYLAMINO)PYRIDIN-2-YL]UREA (3 entities in total)
• 機能のキーワード: hydrolase
• 由来する生物種: HOMO SAPIENS (HUMAN)
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 149267.77

構造登録者

Ruf, A.,Hebeisen, P.,Haap, W.,Kuhn, B.,Mohr, P.,Wessel, H.P.,Zutter, U.,Kirchner, S.,Benz, J.,Joseph, C.,Alvarez-Sanchez, R.,Gubler, M.,Schott, B.,Benardeau, A.,Tozzo, E.,Kitas, E. (登録日: 2011-01-14, 公開日: 2011-05-18, 最終更新日: 2023-12-20)

主引用文献

Hebeisen, P.,Haap, W.,Kuhn, B.,Mohr, P.,Wessel, H.P.,Zutter, U.,Kirchner, S.,Ruf, A.,Benz, J.,Joseph, C.,Alvarez-Sanchez, R.,Gubler, M.,Schott, B.,Benardeau, A.,Tozzo, E.,Kitas, E.
Orally Active Aminopyridines as Inhibitors of Tetrameric Fructose-1,6-Bisphosphatase.
Bioorg.Med.Chem.Lett., 21:3237-, 2011

PubMed Abstract: A novel sulfonylureido pyridine series exemplified by compound 19 yielded potent inhibitors of FBPase showing significant glucose reduction and modest glycogen lowering in the acute db/db mouse model for Type-2 diabetes. Our inhibitors occupy the allosteric binding site and also extend into the dyad interface region of tetrameric FBPase.

PubMed: 21550236
DOI: 10.1016/J.BMCL.2011.04.044

実験手法

X-RAY DIFFRACTION (2.1 Å)