Insight into Binding of Phosphodiesterase-9A Selective Inhibitors by Crystal Structures and Mutagenesis

PDE9 inhibitors have been studied as therapeutics for treatment of cardiovascular diseases, diabetes, and neurodegenerative disorders. To illustrate the inhibitor selectivity, the crystal structures of the PDE9A catalytic domain in complex with the enantiomers of PDE9 inhibitor 1-(2-chlorophenyl)-6-...

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Veröffentlicht in:	Journal of medicinal chemistry 2010-02, Vol.53 (4), p.1726-1731
Hauptverfasser:	Wang, Huanchen, Luo, Xuan, Ye, Mengchun, Hou, Jing, Robinson, Howard, Ke, Hengming
Format:	Artikel
Sprache:	eng
Schlagworte:	3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors 3',5'-Cyclic-AMP Phosphodiesterases - chemistry 3',5'-Cyclic-AMP Phosphodiesterases - genetics 60 APPLIED LIFE SCIENCES AFFINITY Biological and medical sciences CARDIOVASCULAR DISEASES Catalytic Domain CRYSTAL STRUCTURE Crystallography, X-Ray General and cellular metabolism. Vitamins Humans Medical sciences Models, Molecular MUTAGENESIS Mutagenesis, Site-Directed Mutation national synchrotron light source Neuropharmacology Pharmacology. Drug treatments Protein Binding Protein Conformation Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) Psychology. Psychoanalysis. Psychiatry Psychopharmacology Pyrazoles - chemistry Pyrimidines - chemistry RESIDUES SENSITIVITY Stereoisomerism
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