PDE Biology
Cyclic nucleotide phosphodiesterases (PDEs) are important drug targets with unique tissue distribution and functional properties. This family of enzymes is key in the regulation of cyclic nucleotide second messenger levels because they degrade both cAMP and cGMP. Some PDEs hydrolyze both cAMP and cGMP, while others are either cAMP or cGMP hydrolases. Selective PDE inhibitors block the activity of specific PDEs and are used to treat a variety of diseases. Non-selective PDE inhibitors include IBMX and caffeine, both of which are important consumables in basic research laboratories.
Detecting cAMP
cAMP response to isoproterenol followed by inhibition of cAMP production with quinpirole. Detected with the cADDis cAMP assay.
PDE Selectivity Assay
An Optogenetic Tool for Monitoring PDE Rates
The blue-light activated adenylyl cyclase bPAC (#V0100N) can be co-expressed with R-cADDis (#U0200R), a red fluorescent biosensor for cAMP. A two second pulse of blue light activates bPAC to stimulate cAMP production. cAMP degradation by PDE is monitored in real time using R-cADDis. Read about how this method can be used to study the role of PDE activity in neurodegeneration: Live-Cell Assays for Cell Stress Responses Reveal New Patterns of Cell Signaling Caused by Mutations in Rhodopsin, α-Synuclein and TDP-43.
Simple Protocol
Simple, step-by-step protocols for optimizing cAMP and cGMP assays are available online. These assays are non-FRET and cell lysis, enzymes, and co-factors are not necessary. Add our sensors to your cells, incubate, add drug, and measure fluorescence changes.
Sound Intriguing? Get more details on our PDE Biology Assays:
cADDis cAMP Assay
GENIe cGMP Assay
bPAC in BacMam
Recent Publications
- JJ Bakhos, et al. Inhibition of Atrial Natriuretic Peptide Clearance Reduces Myocardial Fibrosis and Improves Cardiac Function in Diabetic Rats. bioRxiv. August 2024.
- RJ Lee, et al. Effects of Akt Activator SC79 on Human M0 Macrophage Phagocytosis and Cytokine Production. Cells. May 2024.
- R. Carey, et al. HSP90 Function is Required for T2R Bitter Taste Receptor Nitric Oxide Production and Innate Immune Responses in Human Airway Epithelial Cells and Macrophages. Cells. April 2022. (bioRxiv)
- I. Gapallawa, et al. Bitter taste receptors stimulate phagocytosis in human macrophages through calcium, nitric oxide, and cyclic-GMP signaling Cell. Mol. Life Sci. Feb, 2020 (bioRxiv)
- J. Wu, et al. Interaction Between HCN and Slack Channels Regulates mPFC Pyramidal Cell Excitability and Working Memory. bioRxiv. March 2023.
- M. Nuriya, et al. Alkyne-Tagged Dopamines as Versatile Analogue Probes for Dopaminergic System Analysis. Analytical Chemistry. July 2021.
- M. Thomas, et al. Optically activated, customizable, excitable cells. PLOS One. December 2020.
- K. Harlen, et al. Live-Cell Assays for Cell Stress Responses Reveal New Patterns of Cell Signaling Caused by Mutations in Rhodopsin, α-Synuclein and TDP-43 Frontiers Cellular Neuroscience. December 2019.
- N. Naim et al. Luminescence-activated nucleotide cyclase regulates spatial and temporal cAMP synthesis. Journal of Biological Chemistry. December 2018.
- Y.A.B. Sierra, et al. Potassium channel-based optogenetic silencing. Nature Communications. November 2018.