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.
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.
Successful drug use in biology and medicine is often prejudiced by the failure of drugs that are otherwise active in vitro to act as efficiently in vivo. This is because in the living animal drugs...
Advances in understanding the molecular mechanisms of disease together with the advent of recombinant DNA and other technologies have opened opportunities for a vast array of novel therapeutic...
PDEs are a family of enzymes that catalyze the hydrolysis of intracellular cyclic nucleotides. They are implicated in a number of disorders and dysfunctions and PDE inhibitors have already proven to...
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