Interested in DNA damage repair pathways for drug discovery? Join us for a live webinar, where Ha Pham, senior scientist at BellBrook Labs, will be sharing her expertise on using the Transcreener ADPR Assay, a biochemical HTS assay, to study enzymes involved in DNA damage repair. She will use CD38 and PARG as target examples for use with the assay. This webinar is free to attend.
Wednesday, May 31st
10:00 AM CDT / 11:00 AM EDT
Duration: 1 hour
Host: Ha Pham Ph.D, Senior Scientist at BellBrook Labs
Poly-ADP-ribosylation is an important posttranslational modification that plays a central role in DNA damage repair (DDR); inhibitors of poly (ADP-ribose) polymerase (PARP) were the first approved drugs targeting DDR. In this webinar, we show how the Transcreener ADPR Assay, a biochemical HTS assay for quantitative measurement of ADP-ribose (ADPR) production, can be used for drug discovery for enzymes that regulate ADP-ribosylation. Cluster of Differentiation 38 (CD38) or CD38 modulates cellular NAD homeostasis by degrading NAD to produce ADPR. It has implications for several pathophysiological conditions including infection, aging, and tumorigenesis. Poly (ADP-ribose) glycohydrolase (PARG) dynamically regulates poly-ADP-ribosylation in concert with PARP by catalyzing the release of ADPR monomers from the polymers. The Transcreener ADPR Assay enables robust, homogenous detection of ADPR formation by PARG and CD38 using a coupling enzyme to convert ADPR into AMP, which is then detected using a far-red, competitive fluorescence polarization (FP) assay. We will show that the assay provides robust signals (>100mP) for initial velocity detection with picomolar concentrations of CD38 and PARG and Z’ values greater than 0.8. Validation studies include a pilot screen of 1280 pharmacologically active molecules and dose response assays to measure the IC50 of confirmed hits. The Transcreener ADPR Assay is a powerful tool for discovery of CD38 and PARG antagonists that will accelerate efforts to modulate DDR pathways therapeutically.
In this webinar, we’ll demonstrate:
- How the Transcreener ADPR Assay will provide a reliable and robust tool for the discovery of CD38 and PARG inhibitors
- The sensitivity and selectivity of the ADPR Assay, and its ability to obtain robust assay signals (>100 mP) for initial velocity detection with picomolar concentrations of CD38 and PARG and Z’ values greater than 0.8
- Validation studies that include a pilot screen of 1280 pharmacologically active molecules and does response assays to measure the IC50 of confirmed hits