Phosphodiesterases (PDEs) are a critical class of enzymes that regulate cellular levels of cyclic nucleotides, such as cAMP and cGMP, by catalyzing their hydrolysis. Dysregulation of PDE activity is associated with a wide range of diseases, including erectile dysfunction, pulmonary hypertension, and neurodegenerative disorders. By targeting specific PDE isoforms with inhibitors, researchers can modulate cyclic nucleotide levels, thereby influencing cellular responses and physiological processes. This makes PDEs an important target in therapeutic development.
We detect PDE hydrolytic activity by monitoring the hydrolysis of phosphodiester bonds in dye-labeled cyclic nucleotides. Following the hydrolysis by PDEs, the resulting nucleotide monophosphate is exposed, allowing for the addition of beads with a high affinity for the monophosphate. This binding interaction alters the motion rate of the fluorescent molecule complex, generating high fluorescence polarization (FP) signal values. The degree of cyclic nucleotide hydrolysis by PDEs, as measured by FP, directly reflects the effectiveness of small molecule inhibitors targeting these enzymes.
PDE Assay Services: We offer a wide range of enzymatic activity assay services for PDE selective inhibitors. They are designed to assess the selectivity of inhibitors across different PDE subtypes, as well as within specific subtypes, such as the multiple targets within the PDE4 subtype.
| Target | Synonyms | Assay Type | Reference Compound |
|---|---|---|---|
| PDE1A | PDE1A5 | Activity | Bay 60-7550 |
| PDE1B | PDE1B1 | Activity | Bay 60-7550 |
| PDE1C | Hcam3 | Activity | Bay 60-7550 |
| PDE2A | Activity | Bay 60-7550 | |
| PDE3A | Activity | Cilostamide, Anagrelide, IBMX, Milrinone | |
| PDE3B | CGIPDE1, CGIP1 | Activity | Cilostamide |
| PDE4A1A | PDE4A1 | Activity | Roflumilast |
| PDE4A4B | PDE4A4, PDE46 | Activity | Roflumilast, BI 1015550 |
| PDE4A10 | Activity | Roflumilast | |
| PDE4B1 | Activity | Roflumilast | |
| PDE4B2 | Activity | Roflumilast, BI 1015550 | |
| PDE4B3 | Activity | Roflumilast | |
| PDE4C1 | Activity | Roflumilast | |
| PDE4C2 | Activity | Roflumilast, BI 1015550 | |
| PDE4D2 | hPDE4D2 | Activity | ML-030, Roflumilast, BI 1015550 |
| PDE4D3 | hPDE4D4 | Activity | ML-030, Roflumilast |
| PDE4D7 | Activity | Roflumilast | |
| PDE5A | PDE5 | Activity | Sildenafil citrate |
| PDE6C | Activity | Sildenafil citrate | |
| PDE7A | HCP1, TM22 | Activity | BRL-50481 |
| PDE7B | bA472E5.1 | Activity | Dipyridamole |
| PDE8A1 | Activity | Dipyridamole | |
| PDE9A2 | Activity | BAY-73-6691 | |
| PDE10A1 | Activity | TP-10 | |
| PDE10A2 | Activity | TP-10 | |
| PDE11A4 | Activity | Dipyridamole |
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