Derecho
Poly(ADP-ribose) polymerases, commonly referred to as PARPs, constitute a significant family of enzymes involved in the regulation of various critical cellular processes, particularly the DNA damage response (DDR) and chromatin structure modifications. The human PARP family consists of seventeen members, each possessing unique regulatory domains while sharing conserved catalytic domains, leading to diverse biological functions and therapeutically applicable targets.
The Role of PARP in Cancer Therapy
In the realm of cancer treatment, the inhibition of PARP1 and PARP2 has emerged as a promising strategy. These inhibitors disrupt single-strand break repair mechanisms in DNA, resulting in synthetic lethality particularly effective in cancers characterized by homologous recombination defects, like BRCA-mutated tumors. Additionally, other PARPs, such as tankyrases, which influence Wnt/β-catenin signaling pathways, expand the potential for new therapeutic avenues within the PARP inhibitor landscape. Comprehensive evaluation of drug candidates necessitates assessing both catalytic inhibition and the capacity of PARP to trap on DNA, which are critical for predicting in vivo activity and safety profiles.
Our Screening Services
Creative Bioarray offers an array of in vitro PARP screening services designed to efficiently evaluate the inhibitory effects of compounds, thereby advancing the early stages of drug discovery:
- Screening for PARP inhibitors
- Single-point concentration and IC50 determination
Assay Details
Biochemical Catalytic Inhibition: Utilizing recombinant PARP enzymes that catalyze the ADP-ribosylation of DNA/protein substrates, our assays are structured to measure inhibitors blocking NAD⁺ consumption or ADP-ribose transfer.
PARP-DNA Trapping (Fluorescence Polarization): This assay monitors fluorescein-labeled DNA duplexes to assess PARP–DNA binding, wherein certain inhibitors enhance the trapping of PARP on DNA, indicated by increased fluorescence polarization signals.
Targets Include:
- PARP1
- PARP2
- PARP3
- PARP6
- PARP7
- PARP10
- Additional targets upon request
Service Highlights
High-throughput Efficiency: Automated platforms enable rapid screening of extensive compound libraries, significantly reducing overall processing time.
Accurate Data Delivery: Our commitment to industry standards ensures that all data generated is reliable and reproducible, accompanied by detailed analytical reports.
Flexible Customization: Tailoring services to meet unique project specifications, whether focused on specific PARP subtypes or varied concentration gradient assessments, is readily available.
Expert Support: Technical assistance is provided to ensure that clients’ specific project needs are addressed throughout the screening process.
Our PARP Screening Services represent a vital resource for your drug discovery initiatives, aiding in the swift identification and refinement of promising PARP inhibitors. For further assistance or to discuss specific project requirements, please reach out to us.