Optimised oligonucleotide substrates to assay XPF-ERCC1 nuclease activity for the discovery of DNA repair inhibitors

We report the design and optimisation of novel oligonucleotide substrates for a sensitive fluorescence assay for high-throughput screening and functional studies of the DNA repair enzyme, XPF-ERCC1, with a view to accelerating inhibitor and drug discovery. Fluorogenic DNA fork substrates have been d...

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Veröffentlicht in:	Chemical communications (Cambridge, England) England), 2019-09, Vol.55 (78), p.11671-11674
Hauptverfasser:	Thomas, Adam M, Brolih, Sanja, McGouran, Joanna F, El-Sagheer, Afaf H, Ptchelkine, Denis, Jones, Morgan, McDonald, Neil Q, McHugh, Peter J, Brown, Tom
Format:	Artikel
Sprache:	eng
Schlagworte:	Design optimization Dimerization DNA Repair DNA-Binding Proteins - chemistry DNA-Binding Proteins - genetics DNA-Binding Proteins - metabolism Endonucleases - chemistry Endonucleases - genetics Endonucleases - metabolism Fluorescence Humans Life Sciences Nuclease Oligonucleotides - chemistry Oligonucleotides - metabolism Repair Substrate Specificity Substrates Temperature
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Beschreibung
Zusammenfassung:	We report the design and optimisation of novel oligonucleotide substrates for a sensitive fluorescence assay for high-throughput screening and functional studies of the DNA repair enzyme, XPF-ERCC1, with a view to accelerating inhibitor and drug discovery. Fluorogenic DNA fork substrates have been designed for use in high-throughput discovery of potential anti-cancer drugs which inhibit DNA repair.
ISSN:	1359-7345 1364-548X
DOI:	10.1039/c9cc05476f