Recently, cilostazol has been proposed for the treatment of diabetic patients and their complications. Cilostazol is a selective inhibitor of phosphodiesterase type 3 that appears to have both antiplatelet and anti-proliferative effects [4]. Cilostazol inhibits platelet aggregation in response to ADP, epinephrine, collagen and arachidonic acid, and suppresses the production of platelet derived ...

A novel bridged nucleic acid (BNA) analogue, 2 0-O,4 0-C-methyleneoxymethylene bridged nucleic acid (2 0,4 0-BNA), was synthesized and incorporated into oligonucleotides. The 2 0,4 0-BNA modified oligonucleotides showed high binding affinity with an RNA complement and significant enzymatic stability against snake venom phosphodiesterase. 2005 Elsevier Ltd. All rights reserved. 2',4'-BNA/LNA (Re...

A genomic DNA fragment from Saccharomyces cerevisiae which contains the SRA5 (=PDE2) gene, coding for a low Km cAMP-phosphodiesterase, was transfected into Chinese hamster ovary cells. Clones carring the cAMP-phosphodiesterase gene were capable of growth in the presence of cholera toxin, which slows the growth of untransfected cells by elevating their cAMP levels. The cholera toxin-resistant tr...

objectives: nitric oxide (no) is a signaling molecule that mediates mechanical bone loading. cyclic guanosine 3', 5' monophosphate (cgmp) is a no-induced effector molecule. the aim of this study was to assess the effect of no-cgmp pathway on orthodontic tooth movement (otm) in rats by use of two phosphodiesterase 5 (pde5) inhibitors namely sildenafil and tadalafil as chemical tools. materials a...

phosphodiesterases  (pde)  hydrolyse intracellular camp  and  cgmp  to  inactive  5’ monophosphates. decreased level of camp is involved in the pathogenesis of asthma. we and others have shown that phosphodiesterases were upregulated in the lung of allergic rats, and bacilli calmette-guérin (bcg) induced the production of camp in vitro. however, it is unclear how bcg’s effect asthma and whether...

Extracts of vegetative cells of Blastocladiella emersonii contain 5% or less of the cyclic AMP phosphodiesterase activity in zoospore extracts. This difference in activity could be accounted for entirely by an increase in the differential rate of phosphodiesterase synthesis during sporulation, beginning after a lag period of about 60 min and extending for at least an additional 90 min into the ...

The calmodulin-activated cyclic nucleotide phosphodiesterase from bovine brain cortex has been extensively purified by two methods, both of which yield preparations containing a single major polypeptide of 58,000 daltons as judged by gel electrophoresis under denaturing conditions. The preparations have similar specific activities in the presence of calmodulin (plus Ca2+) but differ in the degr...

10.2217/14750708.4.2.153 © 2 Isoenzyme phosphodiesterase 4 inhibitors are novel therapeutic agents in late clinical development for the treatment of chronic obstructive pulmonary disease and asthma, both diseases with significant unmet treatment needs. Roflumilast is one such isoenzyme phosphodiesterase 4 inhibitor that is undergoing Phase III clinical development. It is an orally active compou...