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Inhibitors of phosphodiesterase as cancer therapeutics
European Journal of Medicinal Chemistry, 2018Phosphodiesterases (PDEs) are a class of enzymes that hydrolyze cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) which is involved in many physiological processes including visual transduction, cell proliferation and differentiation, cell-cycle regulation, gene expression, inflammation, apoptosis, and metabolic function ...
Lan Bai+7 more
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Chemotherapeutic potential of phosphodiesterase inhibitors
Current Opinion in Chemical Biology, 1998The application of molecular cloning has revealed the phenomenal diversity and complexity of the phosphodiesterase isoenzyme family. Thus, more than 30 human phosphodiesterases are now known; all are apparently necessary for the seemingly simple task of hydrolysing the 3'-ester bond of either cyclic adenosine monophosphate or cyclic guanosine ...
Gerald A Higgs, Martin J Perry
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Phosphodiesterase inhibitors and lung diseases
2023Phosphodiesterase enzymes (PDE) have long been known as regulators of cAMP and cGMP, second messengers involved in various signaling pathways and expressed in a variety of cell types implicated in respiratory diseases such as airway smooth muscle and inflammatory cells making them a key target for the treatment of lung diseases as chronic obstructive ...
Ivana, Stolfa, Clive, Page
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Phosphodiesterase inhibitors in airways disease
European Journal of Pharmacology, 2006Phosphodiesterases hydrolyse intracellular cyclic nucleotides, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) into inactive 5' monophosphates, and exist as 11 families. They are found in a variety of inflammatory and structural cells.
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Phosphodiesterase Inhibitors in Raynaud's Phenomenon
Annals of Pharmacotherapy, 2006Objective: TO evaluate the efficacy of the phosphodiesterase type 5 (PDE5) inhibitors in the treatment of Raynaud's phenomenon. Data Sources: Searches of MEDLINE (1966–March 2006) and Web of Science (1980–March 2006) were conducted; search terms were sildenafil, tadalafil, vardenafil, phosphodiesterase, and Raynaud.
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The Place of Phosphodiesterase Inhibitors
1988Myocardial contractility can be increased by various mechanisms other than those exerted by digitalis or adrenergic agents. The so-called non-digitalis, nonadrenergic agents actually encompass a wide variety of substances among which drugs supposed to act by inhibition of the myocardial phosphodiesterase (type III) appear most promising ...
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A novel insulin secretagogue is a phosphodiesterase inhibitor
Diabetes, 1995The arylpiperazine L-686,398 was described as an oral hypoglycemic agent and is shown to be an insulin secretagogue in vitro. The characteristics of its activity were similar to those of the incretin glucagon-like peptide I (GLP-I). We demonstrate that both the peptide and L-686,398 increase the accumulation of cAMP in isolated ob/ob mouse pancreatic ...
Mark D. Leibowitz+10 more
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Phosphodiesterase inhibitors in the treatment of erectile dysfunction
Drugs of Today, 1998Based on knowledge of intracellular signal propagation in cavernous smooth muscle tone regulation and the development of new and selective pharmacological agents, selective phosphodiesterase (PDE) inhibitors were recently introduced in the treatment of erectile dysfunction.
Truss Mc, Stief Cg
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Pharmacology of Phosphodiesterase Inhibitors
2005The second messengers cyclic 3′,5′ adenosine monophosphate (cAMP) and cyclic 3′,5′ guanosine monophosphate (cGMP) play a key role in mediating a variety of functional responses to hormones and other cellular transmitters. Phosphodiesterases (PDEs) are intracellular enzymes that specifically catalyze the hydrolysis of these second messengers.
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Phosphodiesterase Inhibitors (PDE Inhibitors) and Male Reproduction
2017The nonspecific PDE inhibitors, particularly the methylxanthines: caffeine, pentoxifylline (PTX), and theophylline, are known to stimulate sperm motility in vitro and have been used to treat sperm prior to insemination. The in vivo effects are less dramatic.
Erma Z. Drobnis, Ajay K. Nangia
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