A high-throughput screening dataset of small-molecule inhibitors across human DNA glycosylases
Eddershaw, A.; Dalhus, B.; Gileadi, O.; Graslund, S.; Gunes, I.; Helleday, T.; Liu, K.-C.; Loseva, O.; Nakstad, V. T.; Nilsen, H. L.; Montaldo, N. P.; Nierlin, K.; Norstrom, C.; Rudolfova, N.; Sletta, K.; Sundstrom, M.; Upadhyay, R.; Van Loon, B.; Wigren, E.; Wiita, E.; Wagbo, A. M.; Zhou, K.; Homan, E. J.; Visnes, T.; Michel, M.
Show abstract
The base excision repair pathway removes small base lesions from DNA and is initiated in humans by one of eleven DNA glycosylases with overlapping substrate specificities. Despite their central role in genome maintenance and transcription, systematic datasets describing small-molecule binders or inhibitors of DNA glycosylases are lacking. Here, through a collaborative effort across Scandinavia, we establish a high-throughput biochemical assay platform for human DNA glycosylases and use it to generate a systematic small-molecule screening dataset. A chemogenomic library was screened against nine glycosylases with assays of sufficient quality for hit identification, yielding primary screening and concentration-response data and identifying multiple previously unreported inhibitors. All primary and processed data, along with detailed assay protocols and metadata, are publicly available to support reuse in chemical biology, further compound optimization, assay development and comparative studies of DNA repair enzymes.
Matching journals
The top 2 journals account for 50% of the predicted probability mass.
Similar papers in this journal
- OT-Curtains: an approach for studying protein interactions with DNA-ends using optical tweezers and confocal fluorescence microscopy 92%
- Sequence-directed covalent protein-RNA linkages using engineered HUH-Tags 92%
- Next generation APOBEC3 inhibitors: Optimally designed for potency and nuclease stability 92%
Similar papers in this journal
- Fully computational design of PAM-relaxed Staphylococcus aureus Cas9 with expanded targeting capability 93%
- Uncovering an allosteric mode of action for a selective inhibitor of human Bloom syndrome protein 92%
- Targeting RNA:Protein Interactions with an Integrative Approach Leads tothe Identification of Potent YB-1 Inhibitors 92%
"Similar papers" are the closest papers from that journal in the model's embedding space. They show what the match is built on, but the ranking comes mostly from a classifier over the whole training set, not from these examples alone.