PARPs and PAR Hydrolases

An intricate network of over 150 proteins orchestrate the DNA damage response (DDR). These proteins constantly scan and repair DNA to maintain genome integrity and cellular health in response to DNA lesions caused by normal metabolic activities or by environmental factors such as UV light or radiation.

ADP-ribose Polymerases

Among DDR proteins, ADP-ribose "writers" such as PARPs (Poly ADP-Ribose Polymerases) play prominent roles. The PARP family consists of 17 members, which catalyze the poly- or mono-(ADP-ribosylation) of proteins. The PARP proteins are involved in a wide range of biological functions: DNA repair, chromatin remodeling, mitotic spindle assembly, regulation of RNA turnover, regulation of gene expression, apoptosis, and more. Because of their prominent role in DNA repair and their high expression level compared to other PARP family members, PARP1 and PARP2 are the most extensively studied proteins of the family. Currently approved PARP inhibitors are dual PARP1/PARP2 inhibitors that induce synthetic lethality and have shown great efficacy in some cancers. ​However, inhibition of PARP2 is associated with serious side effects, whereas only PARP1 inhibition is required for synthetic lethality in settings of homologous recombination deficiency. Therefore, the trend is now toward the development of highly selective PARP1 inhibitors.

ADP-ribose Hydrolases

Poly- and mono-ribosylation of DDR proteins is reversed by ADP-ribosylation "erasers" such as PARG (Poly (ADP-ribose) glycohydrolase) and ARH3 (ADP-ribosylhydrolase, also known as ADPRS). The relatively recent development of PARG inhibitors was spurred by the discovery that inhibiting PARG, which results in the accumulation of poly (ADP-ribose) on DDR proteins, induces cancer cell death.

Find a World-Class Suite of Research Tools for PARP Discovery

Biochemical Assays

To facilitate the discovery and development of novel inhibitors, we offer an expansive selection of PARP-specific assay kits, provided in multiple assay formats optimized for various objectives. Whether you are studying the enzymatic activity of a PARP family member, are interested in PARP trapping to DNA, or would like to verify the selectivity of a compound, we have an assay kit for you.

To learn more about PARP/PARG assay kits, visit PARP Assays Page.

Proteins, Cell Lines, Inhibitors, & Services

Bioactive Recombinant Proteins

• Largest commercially available family of active PARPs
• PARG, ARH3 hydrolases
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Knockout Cell Lines

• PARP1 Knockout HeLa Cells
• PARG Knockout HeLa Cells
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Inhibitors

• Single inhibitors to use as control in biochemical or cellular assays
• Set of 8 PARP inhibitors
• ADP-Ribosylation Cycle Inhibitor Cocktails to freeze protein PARylation status in cell lysates
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Custom Development and Services

• PARP/PARPTrap™ Screening and Profiling Services
• Biochemical Assay Development
• Custom Protein Production & Labeling

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