PARP Screening and Profiling Services

BPS is now accepting orders and compounds for our PDE and PARP screening and profiling promotion, a limited time offer. Contact us today for a quote and receive a minimum 10% discount off standard prices. Reference inhibitor is included free of charge on orders of all sizes. Pick and choose any or all PARP/PDE isozymes. Customers under existing contracts are not eligible. 

Our screening services can help accelerate your research and drug discovery programs. These biochemical screens are a fast, reliable, and inexpensive way to identify PARP inhibitors. These assays utilize a histone substrate and biotin-labeled NAD+. Activity is detected by adding Strep-HRP and chemiluminescent or colorimetric substrate (see figure below). BPS Bioscience offers a large variety of PARP related products in addition to our PARP Screening and Profiling Services. Be sure to also look at our immunotherapy-related products and services, as well as our portfolio of kinase products and services.

Trust us to provide you with high quality data with fast turnaround time. Our team of experts along with our broad services portfolio make it easy to:

  • Screen for inhibitors/targets using our PARP assays
  • Select from IC50 determination and single point concentrations
  • Receive data within days of compound submission
  • Perform follow-up studies using the same batches of enzymes manufactured in-house
 

Biochemical Assay Format: 

 

 PARPtrap Assay Format: 

Background: 

Poly (ADP ribose) polymerase, or PARP, is involved in repairing damaged DNA. When DNA is exposed to radiation or toxic chemical compounds, single stranded breaks occur and cause structural damage. PARP recognizes these structural defects, binds to NAD+, and begins to synthesize poly ADP ribose chains. These PAR chains help recruit other repairing enzymes to the site of damage.

PARP inhibition has been implicated as a potential treatment for cancer. Fast growing types of cancer, such as ovarian and prostate cancer, are highly dependent upon PARP. Without PARP to signal for DNA repair, these rapidly growing cancer cells can lyse and die. Also, inhibition of PARP enzymes causes PARP proteins be trapped on the damaged DNA. PARP-DNA complexes can be toxic and prevent cancer cells from proliferating and replicating. BPS Bioscience is the only company that offers a PARPtrap Assay Kit to measure PARP1/DNA complex formation.

There is currently one PARP inhibitor on the market Olaparib (LynparzaTM, AstraZeneca), it was approved by the FDA in 2014 for the treatment of BRCA-mutated ovarian cancer.  Four other PARP inhibitors, niraparib (Tesaro), talazoparib (Medivation), veliparib (AbbVie), and rucaparib (Clovis), are currently in clinical trials for the treatment of breast cancer and ovarian cancer among others.

In addition to PARP inhibition, immunotherapy, named by Science magazine as Breakthrough of the Year in 2013, has emerged as a successful form of treatment for cancer. According to the Journal of Cancer Immunology Research, PARP inhibitors can be used for successful cytotoxic therapy and when administered with CTLA-4 blockers, PARP inhibitors increase survival rates and activate the immune system to destroy tumor cells.

Not only are PARP inhibitors being investigated as combination therapies with immune checkpoint inhibitors, but recent data also suggests that PARP inhibitors can have powerful anti-cancer effects when used in combination with PI3K or Wee1 inhibitors. Like PARP inhibitors, PI3K inhibition results in increased DNA damage and combinations increase cancer cell synthetic lethality. Wee1 inhibitors cause abrogation of radiation-induced G2 checkpoint and impaired homologous recombination repair (HRR). Combining Wee1 and PARP inhibitors produces significantly more radiosensitization in in vitro and in vivo pre-clinical models of cancer.

 

Get Started:

Fill out the Compound Submission Form and include it with your compounds when shipping in addition to emailing it to the email address provided on the form. 

When mailing compounds, follow these detailed shipping instructions

Please note: In order to minimize the turnaround time for service orders, please fill out the Compound Submission Form as completely as possible. Failure to include a Compound Submission Form with accurate and complete information will result in delayed screens.