Open Screening Dataset Maps Small-Molecule Inhibitors Across Nine Human DNA Glycosylases
- A Scandinavian consortium built a high-throughput biochemical assay platform for human DNA glycosylases, the eleven enzymes that initiate base excision repair.
- A chemogenomic library was screened against nine glycosylases with assays good enough for hit calling, yielding primary and concentration-response data and several previously unreported inhibitors.
- All data, protocols and metadata are publicly available.
💡 Points
Glycosylases have been chemically neglected, so an open, annotated screen across nine of them is starting material a hit-finding team can mine directly. Chemogenomic libraries carry target annotations, which helps with mechanism and selectivity reads. I'd immediately cross-check the hits for assay interference and DNA-binder artifacts, since nucleic-acid enzyme screens are notorious for them.
A high-throughput screening dataset of small-molecule inhibitors across human DNA glycosylases ↗