On Demand Webinar: Development of Ectonucleotidase Assay Methods Using the Transcreener® HTS Assay Platform
View the Webinar On Demand at Anytime
Ectonucleotidases are plasma membrane-bound enzymes with externally oriented active sites that metabolize nucleotides to nucleosides. One example is ectonucleoside triphosphate diphosphohydrolase-1, also known as CD39, ENTPD1, or NTPDase1. CD39 hydrolyzes ATP and ADP to AMP. Other ectonucleotidases such as CD73 process the AMP further into adenosine, which is an important signaling molecule for immunosuppression in the tumor microenvironment. For this reason, ectonucleotidases are emerging as promising immuno-oncology targets, with a number of groups working on small molecule and antibody-based inhibitors. As the only HTS method capable of direct detection of nucleotides, the Transcreener® platform is uniquely suited for measuring ectonucleotidase activity with the high sensitivity and low levels of interference required for a successful HTS campaign.
In this webinar we discussed:
- CD39 Assay development for using the Transcreener® AMP2/GMP2 Assay with fluorescence polarization and TR-FRET readouts
- Demonstrated assay robustness for use in high-throughput screening
- Inhibitor potency profiling for CD39
- Recent external publications using Transcreener® HTS assays for studying ectonucleotidase activity
