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Title Phosphodiesterases as drug targets / Sharron H. Francis, Marco Conti, Miles D. Houslay, editors.
Imprint Berlin ; New York : Springer, ©2011.


 Internet  Electronic Book    AVAILABLE
Description 1 online resource (xvii, 519 pages)
Series Handbook of experimental pharmacology ; v. 204
Handbook of experimental pharmacology ; v. 204.
Bibliog. Includes bibliographical references and index.
Note Available only to authorized UTEP users.
Print version record.
Subject Drug targeting.
Phosphoric Diester Hydrolases -- therapeutic use.
Drug Discovery.
Phosphodiesterase Inhibitors -- pharmacology.
Phosphodiesterase Inhibitors -- therapeutic use.
Phosphoric Diester Hydrolases -- pharmacology.
Contents Phosphodiesterase inhibitors: history of pharmacology -- Phosphodiesterase inhibitors: factors that influence potency, selectivity, and action -- Pharmacology, clinical efficacy, and tolerability of phosphodiesterase-4 inhibitors: impact of human pharmacokinetics -- Structural insight into the substrate specificity of phosphodiesterases -- Fission yeast-based platform for phosphodiesterase inhibitor HTSs and analysis of phosphodiesterase activity -- GAF-tandem domain of phosphodiesterase 5 as a potential drug target -- Small molecule allosteric modulators of phosphodiesterase 4 -- Regulation of endothelial barrier function by cyclic nucleotides: the role of phosphodiesterases -- Phosphodiesterases as targets for intermittent claudication -- Phosphodiesterase inhibition in heart failure -- Phosphodiesterases: emerging therapeutic targets for neonatal pulmonary hypertension -- Role of phosphodiesterases in adult-onset pulmonary artery hypertension -- Treatment of erectile dysfunction -- and lower urinary tract symptoms by phosphodiesterase inhibitors -- Evaluation of the therapeutic utility of phosphodiesterase 5A inhibition in the mdx mouse model of Duchenne muscular dystrophy -- Phosphodiesterases as targets for modulating t-cell responses -- Cyclic nucleotides and phosphodiesterases in monocytic differentiation -- Phosphodiesterase inhibitors in the treatment of inflammatory diseases -- Harnessing the clinical efficacy of phosphodiesterase 4 inhibitors in inflammatory lung diseases: dual-selective phosphodiesterase inhibitors and novel combination therapies -- Phosphodiesterases in the central nervous system: implications in mood and cognitive disorders -- Therapeutic potential of phosphodiesterase inhibitors in parasitic diseases.
Summary Cyclic nucleotide phosphodiesterases (PDEs) are promising targets for pharmacological intervention. Multiple PDE genes, isoform diversity, selective expression and compartmentation of the isoforms, and an array of conformations of PDE proteins are properties that challenge development of drugs that selectively target this class of enzymes. Novel characteristics of PDEs are viewed as unique opportunities to increase specificity and selectivity when designing novel compounds for certain therapeutic indications. This chapter provides a summary of the major concepts related to the design and use of PDE inhibitors.
Other Author Francis, Sharron H.
Conti, Marco.
Houslay, Miles D.
Other Title Springer eBooks
Printed edition: 9783642179686