Cyclic Nucleotide Phosphodiesterases (PDEs)

Cyclic nucleotide phosphodiesterases (PDEs) are ubiquitously distributed throughout mammalian tissues and play a major role in cell signaling by hydrolyzing cAMP and/or cGMP. Due to their diversity and specific distribution at the cellular and subcellular levels, PDEs are able to selectively regulate various cellular functions. This regulatory ability implicates PDEs in various therapeutic areas including CNS, inflammation, and oncology.
 
As PDEs are expressed in a variety of tissues, selectivity is a prerequisite for a therapeutically viable PDE inhibitor. For example, high selectivity for PDE5 inhibitors is important for treating erectile dysfunction while minimizing possible side effects associated with the inhibition of other PDEs. These possible side effects include tachycardia and vasodilation that are attributed to inhibition of PDE1 and PDE3, or blue-green vision disturbances that are attributed to inhibition of PDE6.
 
In order to meet the growing need for robust PDE profiling, Eurofins Discovery has designed a HTS platform of assays to determine the inhibitory effects and selectivity of compounds on the PDE superfamily.