title: Cyclic nucleotide phosphodiesterase assay technology.
abstract: Because of their critical role in modulating cellular cyclic nucleotide levels, phosphodiesterases (PDEs) are involved in many disease-related signaling pathways. The PDE family is large and diverse, with members having different tissue distribution, sub-cellular localizations, and substrate specificities. Because of these characteristics, the PDEs represent a broad group of potential drug targets. Described in the present unit are the assay development and validation procedures needed to establish a high-throughput screening system for these important enzymes. The assays provide a structured approach for determining the kinetic parameters of related enzyme families to facilitate the characterization of PDE inhibitors.
authors.affiliation: Scottish Biomedical, Glasgow, Scotland, United Kingdom.
authors.forename: S J
authors.initials: SJ
authors.lastname: MacKenzie
authors.forename: S F
authors.initials: SF
authors.lastname: Hastings
authors.forename: C
authors.initials: C
authors.lastname: Wells
mesh_terms: D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors / Q000378:metabolism*; D015106:3',5'-Cyclic-GMP Phosphodiesterases / Q000037:antagonists & inhibitors / Q000378:metabolism*; D002846:Chromatography, Affinity / Q000379:methods; D057075:Enzyme Assays / Q000379:methods*; D006801:Humans; D006868:Hydrolysis; D011869:Radioligand Assay / Q000379:methods*; D013048:Specimen Handling / Q000379:methods; D013379:Substrate Specificity; D017186:Titrimetry / Q000379:methods
chemical_list: D015105:3',5'-Cyclic-AMP Phosphodiesterases; D015106:3',5'-Cyclic-GMP Phosphodiesterases