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- Ekblad, Torun (author)
Identification of Poly(ADP-Ribose) Polymerase Macrodomain Inhibitors Using an AlphaScreen Protocol
- Article/chapterEnglish2018
Publisher, publication year, extent ...
- Sage Publications,2018
- printrdacarrier
Numbers
- LIBRIS-ID:oai:DiVA.org:umu-147337
- https://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-147337URI
- https://doi.org/10.1177/2472555217750870DOI
- http://kipublications.ki.se/Default.aspx?queryparsed=id:138079022URI
Supplementary language notes
- Language:English
- Summary in:English
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- SwePubSwePub
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Notes
- Macrodomains recognize intracellular adenosine diphosphate (ADP)-ribosylation resulting in either removal of the modification or a protein interaction event. Research into compounds that modulate macrodomain functions could make important contributions. We investigated the interactions of all seven individual macrodomains of the human poly(ADP-ribose) polymerase (PARP) family members PARP9, PARP14, and PARP15 with five mono-ADP-ribosylated (automodified) ADP-ribosyltransferase domains using an AlphaScreen assay. Several mono-ADP-ribosylation-dependent interactions were identified, and they were found to be in the micromolar affinity range using surface plasmon resonance (SPR). We then focused on the interaction between PARP14 macrodomain-2 and the mono-ADP-ribosylated PARP10 catalytic domain, and probed a similar to 1500-compound diverse library for inhibitors of this interaction using AlphaScreen. Initial hit compounds were verified by concentration-response experiments using AlphaScreen and SPR, and they were tested against PARP14 macrodomain-2 and -3. Two initial hit compounds and one chemical analog each were further characterized using SPR and microscale thermophoresis. In conclusion, our results reveal novel macrodomain interactions and establish protocols for identification of inhibitors of such interactions.
Subject headings and genre
- MEDICIN OCH HÄLSOVETENSKAP Medicinsk bioteknologi Medicinsk bioteknologi hsv//swe
- MEDICAL AND HEALTH SCIENCES Medical Biotechnology Medical Biotechnology hsv//eng
- ADP-ribosylation
- macrodomain inhibitor
- PARP
- protein-protein interaction
- AlphaScreen
Added entries (persons, corporate bodies, meetings, titles ...)
- Verheugd, Patricia (author)
- Lindgren, Anders E.Umeå universitet,Kemiska institutionen(Swepub:umu)arslin04 (author)
- Nyman, TomasKarolinska Institutet (author)
- Elofsson, MikaelUmeå universitet,Kemiska institutionen(Swepub:umu)miel0001 (author)
- Schüler, HerwigKarolinska Institutet (author)
- Umeå universitetKemiska institutionen (creator_code:org_t)
Related titles
- In:SLAS Discovery: Sage Publications23:4, s. 353-3622472-55602472-5552
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