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Phosphodiesterases as Drug Targets de Sharron H. Francis

Phosphodiesterases as Drug Targets: Handbook of Experimental Pharmacology, cartea 204

Editat de Sharron H. Francis, Marco Conti, Miles D. Houslay
en Limba Engleză Paperback – 26 noi 2013
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.
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Specificații

ISBN-13: 9783642269455
ISBN-10: 3642269451
Pagini: 540
Ilustrații: XVIII, 522 p.
Dimensiuni: 155 x 235 x 28 mm
Greutate: 0.75 kg
Ediția:2011
Editura: Springer Berlin, Heidelberg
Colecția Springer
Seria Handbook of Experimental Pharmacology

Locul publicării:Berlin, Heidelberg, Germany

Public țintă

Research

Cuprins

Phosphodiesterase inhibitors: History of pharmacology; PDE inhibitors: factors that influence potency, selectivity and action; A fission yeast-based platform for phosphodiesterase inhibitor high throughput screening and analyses of phosphodiesterase activity; The pharmacokinetics of PDE inhibitors and the impact of this on their efficacy and the therapeutic window; Structural insight into the substrate specificity of phosphodiesterases;The GAF-tandem domain of phosphodiesterase 5 as a potential drug target; Small molecule allosteric modulators of phosphodiesterase 4; PDE 2 holoenzyme-insights about full length PDE and mechanism of activation by cGMP binding; Harnessing the clinical efficacy of phosphodiesterase 4 inhibitors in inflammatory lung diseases with dual-selective phosphodiesterase inhibitors and novel combination therapies; PDE inhibitors in the treatment of inflammatory diseases; Cyclic nucleotides and phosphodiesterases in monocyte differentiation; PDEs as targets for modulating T cell responses; Role of PDEs in adult-onset pulmonary arterial hypertension; Phosphodiesterases: emerging therapeutic targets for neonatal pulmonary hypertension; Phosphodiesterase inhibition in heart failureEvaluation of the Therapeutic Utility of Phosphodiesterase 5A Inhibition in the mdx MouseModel of Duchenne Muscular Dystrophy; PDEs as targets for intermittent claudication; Treatment of erectile dysfunction and lower urinary tract symptoms by phosphodiesteraseinhibitors; Regulation of endothelial barrier function by cyclic nucleotides: the role of phosphodiesterases; Potential use of PDE inhibitors in treatment of depression and improvement of cognition; PDEs as targets for the treatment of basal ganglia disordersTherapeutic potential of PDE inhibitors in parasitic diseases

Textul de pe ultima copertă

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.

Caracteristici

provides a summary of the major concepts related to the design and use of PDE inhibitors describes exciting ideas and developments that are currently emerging in this dynamic and important field written by leading authorities in the field Includes supplementary material: sn.pub/extras