3GOI

Human glucokinase in complex with a synthetic activator

3GOI の概要

• エントリーDOI: 10.2210/pdb3goi/pdb
• 分子名称: Glucokinase, alpha-D-glucopyranose, 2-(methylamino)-N-(4-methyl-1,3-thiazol-2-yl)-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]benzamide, ... (4 entities in total)
• 機能のキーワード: glucokinase, diabetes, allosteric activator, atp-binding, glycolysis, kinase, nucleotide-binding, transferase
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 51519.52

構造登録者

Kamata, K.,Mitsuya, M. (登録日: 2009-03-19, 公開日: 2009-04-28, 最終更新日: 2024-03-20)

主引用文献

Mitsuya, M.,Kamata, K.,Bamba, M.,Watanabe, H.,Sasaki, Y.,Sasaki, K.,Ohyama, S.,Hosaka, H.,Nagata, Y.,Eiki, J.,Nishimura, T.
Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators
Bioorg.Med.Chem.Lett., 19:2718-2721, 2009

PubMed Abstract: A novel class of 3,6-disubstituted 2-pyridinecarboxamide derivatives was designed based on X-ray analysis of the 2-aminobenzamide lead class. Subsequent chemical modification led to the discovery of potent GK activators which eliminate potential toxicity concerns associated with an aniline group of the lead structure. Compound 7 demonstrated glucose lowering effect in a rat OGTT model.

PubMed: 19362831
DOI: 10.1016/j.bmcl.2009.03.137

実験手法

X-RAY DIFFRACTION (2.52 Å)