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Phosphodiesterases as therapeutic targets
Urology, 2003The advent of sildenafil (Viagra) for the treatment of erectile dysfunction has attracted widespread interests in phosphodiesterase type 5 (PDE5), the target of sildenafil, 1 and other members of the PDE superfamily. PDEs are intracellular enzymes that catalyze the hydrolysis of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate ...
Guiting Lin +3 more
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Phosphodiesterase-5 Inhibitors
2013Nitric oxide (NO) signaling plays a key role in modulating vascular tone and remodeling in the pulmonary circulation. The guanylate cyclase/cyclic guanylate monophosphate-signaling pathway primarily mediates nitric oxide signaling. This pathway is critical in normal regulation of the pulmonary vasculature, and is an important target for therapy in ...
Barbara A. Cockrill, Aaron B. Waxman
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Phosphodiesterase 4 inhibitors
Journal of the American Academy of Dermatology, 2018Historically, drugs available for treating atopic dermatitis (AD) have been limited to topical corticosteroids and topical calcineurin inhibitors, with systemic immunosuppressants and phototherapy reserved for severe AD. Despite their efficacy and infrequent adverse events, phobia about the use of topical steroids and calcineurin inhibitors has limited
Rema Zebda, Amy S. Paller
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1999
Airway obstruction and hyperreactivity in asthma are mainly caused by accumulation of inflammatory cells and their mediators promoting bronchoconstriction, airway oedema and airway remodeling. Cyclic AMP counteracts a huge variety of inflammatory cell functions involved in the development and maintenance of asthma.
Christian Schudt, Hermann Tenor
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Airway obstruction and hyperreactivity in asthma are mainly caused by accumulation of inflammatory cells and their mediators promoting bronchoconstriction, airway oedema and airway remodeling. Cyclic AMP counteracts a huge variety of inflammatory cell functions involved in the development and maintenance of asthma.
Christian Schudt, Hermann Tenor
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Xanthines and Phosphodiesterase Inhibitors
2016Theophylline is an orally acting xanthine that has been used since 1937 for the treatment of respiratory diseases including asthma and chronic obstructive pulmonary disease (COPD). However, in most treatment guidelines, xanthines have now been consigned to third-line therapy because of their narrow therapeutic window and propensity for drug-drug ...
Clive P. Page, Domenico Spina
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An update on phosphodiesterase (PDE) inhibitors: Phosphodiesterases and drug selectivity
Methods and Findings in Experimental and Clinical Pharmacology, 2005In recent years, there has been a prodigious expansion of knowledge about cyclic nucleotide phosphodiesterases (PDEs). This isozyme superfamily has now become a major focus of drug discovery efforts owing to its diversity, molecular nature, differential regulation and expression in different cell types, and the range of biological functions. Inhibition
Kumar G, Kumar Rs, Gupta R
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Pulmonary Responses to Selective Phosphodiesterase-5 and Phosphodiesterase-3 Inhibitors
Chest, 2004To compare the direct pulmonary vasodilating activity and specificity of phosphodiesterase-5 (zaprinast) and phosphodiesterase-3 (milrinone) inhibitors on the pulmonary vascular (PV) bed of the spontaneously breathing cat with an intact chest.Prospective, randomized animal study.Laboratory of university hospital.Experiments were performed in vivo in ...
Yaacov Gozal, Idit Matot
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Carboxyamidotriazole: A novel inhibitor of both cAMP-phosphodiesterases and cGMP-phosphodiesterases
European Journal of Pharmacology, 2015Carboxyamidotriazole (CAI) is a non-cytotoxic anti-tumor drug, which also shows considerable anti-inflammatory effects in a variety of animal models of inflammation. The exact target and mechanism of CAI were not clearly understood yet. In the present study, we demonstrate that CAI is a non-selective phosphodiesterase (PDE) inhibitor, which provides ...
Lei Guo +8 more
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2007
This chapter provides a thorough examination of the state of the art of phosphodiesterase enzymes (PDEs) and published inhibitors. There are a total of 11 known types of PDEs in the superfamily, PDE1–PDE11, and, within this group, there are a variety of subtypes and isoforms, some of which have unique function(s).
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This chapter provides a thorough examination of the state of the art of phosphodiesterase enzymes (PDEs) and published inhibitors. There are a total of 11 known types of PDEs in the superfamily, PDE1–PDE11, and, within this group, there are a variety of subtypes and isoforms, some of which have unique function(s).
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Cyclic nucleotide phosphodiesterases
Journal of Allergy and Clinical Immunology, 2001Cyclic nucleotide second messengers (cAMP and cGMP) play a central role in signal transduction and regulation of physiologic responses. Their intracellular levels are controlled by the complex superfamily of cyclic nucleotide phosphodiesterase (PDE) enzymes. Continuing advances in our understanding of the molecular pharmacology of these enzymes has led
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