5XKM

Crystal structure of human phosphodiesterase 2A in complex with 6-methyl-N-(1-(4-(trifluoromethoxy)phenyl)propyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide

5XKM の概要

• エントリーDOI: 10.2210/pdb5xkm/pdb
• 分子名称: cGMP-dependent 3',5'-cyclic phosphodiesterase, MAGNESIUM ION, ZINC ION, ... (5 entities in total)
• 機能のキーワード: hydrolase, hydrolase inhibitor, pde2a
• 由来する生物種: Homo sapiens (Human)
• 細胞内の位置: Isoform PDE2A3: Cell membrane ; Lipid-anchor . Isoform PDE2A2: Mitochondrion matrix . Isoform PDE2A1: Cytoplasm . Isoform 5: Mitochondrion : O00408
• タンパク質・核酸の鎖数: 6
• 化学式量合計: 244249.29

構造登録者

Oki, H.,Kondo, M.,Snell, G.,Lane, W. (登録日: 2017-05-08, 公開日: 2017-08-16, 最終更新日: 2024-03-27)

• 主引用文献: Mikami, S.,Sasaki, S.,Asano, Y.,Ujikawa, O.,Fukumoto, S.,Nakashima, K.,Oki, H.,Kamiguchi, N.,Imada, H.,Iwashita, H.,Taniguchi, T.; Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders.; J. Med. Chem., 60:7658-7676, 2017; PubMed: 28759228; DOI: 10.1021/acs.jmedchem.7b00709

実験手法

X-RAY DIFFRACTION (2.16 Å)