Poly (ADP-ribose) polymerases (PARPs) represent a crucial family of enzymes involved in the ADP-ribosylation modification using NAD⁺ as a substrate. These enzymes play significant roles in overseeing DNA damage repair, chromatin architecture, and regulation of transcription. Among the 17 human PARP family members, their catalytic domains are conserved, yet each has distinct regulatory functions, leading to varied biological implications and the potential for therapeutic targeting.
PARP Inhibition and Cancer Treatment
The therapeutic inhibition of PARP1 and PARP2 disrupts single-strand break repair mechanisms, leading to synthetic lethality particularly in cancers with homologous recombination deficiencies, such as BRCA-mutated tumors. This unique characteristic has made PARP inhibitors effective agents in cancer treatment. Additionally, enzymes such as tankyrases (PARP5a and PARP5b), which modulate Wnt/β-catenin signaling and cellular proliferation, further widen the spectrum of PARP targets for therapeutic intervention.
Our Comprehensive PARP Screening Services
Creative Bioarray offers in vitro PARP screening services specifically designed to facilitate the assessment of your compound’s inhibitory potential, thus accelerating your drug discovery process. Our services include:
- Screening for PARP inhibitors
- IC50 determination and single-point concentration testing
Assay Details
- Biochemical catalytic inhibition: The catalytic activity of recombinant PARP enzymes leads to the ADP-ribosylation of DNA or protein substrates. Inhibitory compounds either obstruct NAD⁺ consumption or hinder the transfer of ADP-ribose.
- PARP-DNA Trapping (Fluorescence Polarization): Utilizing fluorescently labeled DNA duplex, we monitor PARP-DNA binding, noting that some inhibitors promote enhanced PARP “trapping” on DNA, as indicated by an increased fluorescence polarization signal.
List of Target Enzymes
| PARP Members | |||
|---|---|---|---|
| PARP1 | PARP7 | PARP12 | PARP5B |
| PARP2 | PARP8 | PARP14 | PARG |
| PARP3 | PARP10 | PARP15 | ARH3 |
| PARP6 | PARP11 | PARP5a |
Additional members of the PARP family can be included upon request.
Service Highlights
- High-throughput capabilities: Our automated platforms enable rapid screening of numerous compound samples, significantly reducing screening time.
- Accuracy and reliability: We adhere to rigorous industry standards, employing validated methods to ensure reproducibility in results.
- Customization: Our services are adaptable to meet specific project requirements, whether targeting specific PARP subtypes or varying concentration gradients.
- Expert support: Our experienced team is available to tailor our services to your project’s unique needs.
Conclusion
Our PARP Screening Services serve as an essential component of your drug discovery efforts, assisting in the rapid identification and optimization of promising PARP inhibitors. To learn more about how we can enhance your research initiatives, please reach out to our team for further information.
