3B2R

Crystal Structure of PDE5A1 catalytic domain in complex with Vardenafil

3B2R の概要

• エントリーDOI: 10.2210/pdb3b2r/pdb
• 分子名称: cGMP-specific 3',5'-cyclic phosphodiesterase, 2-{2-ETHOXY-5-[(4-ETHYLPIPERAZIN-1-YL)SULFONYL]PHENYL}-5-METHYL-7-PROPYLIMIDAZO[5,1-F][1,2,4]TRIAZIN-4(1H)-ONE (3 entities in total)
• 機能のキーワード: cgmp phosphodiesterase; pde5-inhibitor potency; vardenafil; sildenafil; levitratm., allosteric enzyme, alternative splicing, cgmp-binding, hydrolase, magnesium, metal-binding, nucleotide-binding, phosphorylation, polymorphism, zinc
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 77381.21

構造登録者

Huanchen, W.,Mengchun, Y.,Howard, R.,Sharron, H.F.,Hengming, K. (登録日: 2007-10-19, 公開日: 2008-05-20, 最終更新日: 2024-04-03)

• 主引用文献: Wang, H.,Ye, M.,Robinson, H.,Francis, S.H.,Ke, H.; Conformational variations of both phosphodiesterase-5 and inhibitors provide the structural basis for the physiological effects of vardenafil and sildenafil.; Mol.Pharmacol., 73:104-110, 2008; PubMed: 17959709; DOI: 10.1124/mol.107.040212

実験手法

X-RAY DIFFRACTION (2.07 Å)