We have developed two assays to detect therapeutic enzyme targets, including phosphodiesterases and cyclases. Both are homogeneous, highly sensitive and non-radioactive luminescence-based assays with significant relevance to drug discovery.
Cell culture assays for the detection of phosphodiesterase (PDE) are essential for reliable HTS. PDE is a group of enzymes that break down two of the most important signaling molecules in cells, cAMP and cGMP, which underlie many cellular processes crucial to our health. As such, PDE is a crucial therapeutic target. PDE-targeted drugs already provide treatment for various diseases, including neurodegenerative disorders4 and heart failure.5 PDEs are also associated with off-target side effects of various drugs6, so profiling PDE is also crucial step in the development of both PDE- and non-PDE-targeted drugs. Our PDELightTM HTS cAMP Phosphodiesterase Bioassay Kit provides a simple, robust and rapid measurement of phosphodiesterase (PDE) activity. When PDE is present, it breaks down cAMP into AMP, which is converted into ATP. The PDELightTM Assay Kit uses bioluminescent detection of this ATP in your cell cultures, emitting nearly one photon of light for every ATP molecule produced. If you’d like to learn more or request a quote, visit the PDELightTM HTS cAMP Phosphodiesterase Assay Kit product page.
Identifying the presence of inorganic pyrophosphate (PPi) is vital for HTS drug discovery. PPi is a small molecule generated from a variety of enzymes, including from cyclases. Cyclases have key regulatory roles in all cells and underlie various pathologies, such as obesity and cardiopulmonary disease, stimulating the development of various cyclase-targeting drugs. Some cyclases, such as adenylyl cyclases, could also be useful drug targets themselves.7
Our PPiLightTM Inorganic Pyrophosphate Bioassay offers a versatile, simple (two-step) and fast method for identifying PPi using a bioluminescent marker. In the presence of PPi, the detection reagent catalyzes the conversion of AMP into ATP. The PPiLightTM Assay uses luciferase to produce light from the newly formed ATP and luciferin, offering a wide detection range from 0.02µM to 10 µM. As well as its application in the measurement of cyclases, the PPiLightTM Assay can also measure the activity of various other clinically relevant enzymes, including phosphotransferases, pyrophosphotases, ligases, hydrolases and DNA Polymerases.
If you’d like to learn more or request a quote, visit the PPiLightTM Inorganic Pyrophosphate Bioassay product page.