A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function

• Published in: Bioorganic & medicinal chemistry letters Vol. 16; no. 3; pp. 718 - 721
• Main Authors: Chambers, Robert J., Abrams, Kristin, Castleberry, Tessa A., Cheng, John B., Fisher, Douglas A., Kamath, Ajith V., Marfat, Anthony, Nettleton, David O., Pillar, Joann D., Salter, Eben D., Sheils, Alissa L., Shirley, John T., Turner, Claudia R., Umland, John P., Lam, Kelvin T.
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 01.02.2006; Elsevier
• Subjects: 3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors; 3',5'-Cyclic-AMP Phosphodiesterases - physiology; Analytical, structural and metabolic biochemistry; Biological and medical sciences; Chemotaxis - drug effects; Cyclic Nucleotide Phosphodiesterases, Type 4; Enzymes and enzyme inhibitors; Eosinophil; Eosinophils - drug effects; Eosinophils - physiology; Fundamental and applied biological sciences. Psychology; Hydrolases; Isoenzymes - antagonists & inhibitors; Isoenzymes - chemistry; Isoenzymes - metabolism; Leukocytes - drug effects; Leukocytes - physiology; Medical sciences; Miscellaneous; Niacinamide - antagonists & inhibitors; PDE4D; Pharmacology. Drug treatments; Phosphodiesterase; Phosphodiesterase Inhibitors - chemistry; Phosphodiesterase Inhibitors - pharmacology; Rolipram - chemistry; Rolipram - pharmacology; PDE4D; Eosinophil; Phosphodiesterase; Human; 3',5'-Cyclic-nucleotide phosphodiesterase; Enzyme; Nitrogen heterocycle; Isozyme; Enzyme inhibitor; Esterases; Selectivity; Phosphoric diester hydrolases; Chemotaxis; In vitro; Thiophene derivatives; Rolipram; Six membered ring; Hydrolases; Carboxamide; Fluorine Organic compounds; Mechanism of action; Comparative study; Release
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2005.10.026

Nicotinamide ( 2) is a potent and selective inhibitor of the PDE4D isozyme and as a chemical tool selectively blocks eosinophil mediator release and chemotaxis thus linking the role of PDE4D to eosinophil function. Nicotinamide ( 2) is a potent and selective inhibitor of the PDE4D isozyme and as a chemical tool selectively blocks eosinophil mediator release and chemotaxis thus linking the role of PDE4D to eosinophil function.