Abstract
Mono-ADP-ribosyltransferases of the PARP/ARTD enzyme family are enzymes catalyzing the transfer of a single ADP-ribose unit to target proteins. The enzymes have various roles in vital cellular processes such as DNA repair and transcription, and many of the enzymes are linked to cancer-relevant functions. Thus inhibition of the enzymes is a potential way to discover and develop new drugs against cancer. Here we describe an activity-based screening assay for mono-ADP-ribosyltransferases. The assay utilizes the natural substrate of the enzymes, NAD<sup>+</sup>, and it is based on chemically converting the leftover substrate to a fluorophore and measuring its relative concentration after the enzymatic reaction. The assay is homogenous, robust, and cost-effective and, most importantly, applicable to mono-ADP-ribosyltransferases as well as poly-ADP-ribosyltransferases for screening of small-molecule inhibitors against the enzymes.
| Original language | English |
|---|---|
| Title of host publication | ADP-ribosylation and NAD+ Utilizing Enzymes |
| Subtitle of host publication | Methods and Protocols |
| Publisher | Springer |
| Pages | 237-244 |
| Number of pages | 8 |
| ISBN (Electronic) | 978-1-4939-8588-3 |
| ISBN (Print) | 978-1-4939-8587-6, 978-1-4939-9335-2 |
| DOIs | |
| Publication status | Published - 1 Jan 2018 |
| MoE publication type | A3 Part of a book or another research book |
UN SDGs
This output contributes to the following UN Sustainable Development Goals (SDGs)
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SDG 3 Good Health and Well-being
Keywords
- ARTD
- Inhibitor
- Mono-ADP-ribosyltransferase
- PARP
- Screening assay
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