A high-throughput screening dataset of small-molecule inhibitors across human DNA glycosylases
- 1Karolinska Institutet
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.
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BibTeX
@misc{eddershaw2026highthroughput,
title = {{A high-throughput screening dataset of small-molecule inhibitors across human DNA glycosylases}},
author = {A. Eddershaw and B. Dalhus and O. Gileadi and S. Graslund and I. Gunes and T. Helleday and K.-C. Liu and O. Loseva and V. T. Nakstad and H. L. Nilsen and N. P. Montaldo and K. Nierlin and C. Norstrom and N. Rudolfova and K. Sletta and M. Sundstrom and R. Upadhyay and B. Van Loon and E. Wigren and E. Wiita and A. M. Wagbo and K. Zhou and E. J. Homan and T. Visnes and M. Michel},
howpublished = {bioRxiv},
year = {2026},
month = sep,
doi = {10.64898/2026.09.25.752594},
url = {https://www.biorxiv.org/content/10.64898/2026.09.25.752594v1},
note = {CC BY},
}
RIS
TY - UNPB
TI - A high-throughput screening dataset of small-molecule inhibitors across human DNA glycosylases
AU - A. Eddershaw
AU - B. Dalhus
AU - O. Gileadi
AU - S. Graslund
AU - I. Gunes
AU - T. Helleday
AU - K.-C. Liu
AU - O. Loseva
AU - V. T. Nakstad
AU - H. L. Nilsen
AU - N. P. Montaldo
AU - K. Nierlin
AU - C. Norstrom
AU - N. Rudolfova
AU - K. Sletta
AU - M. Sundstrom
AU - R. Upadhyay
AU - B. Van Loon
AU - E. Wigren
AU - E. Wiita
AU - A. M. Wagbo
AU - K. Zhou
AU - E. J. Homan
AU - T. Visnes
AU - M. Michel
PY - 2026
DA - 2026/09/25
PB - bioRxiv
DO - 10.64898/2026.09.25.752594
UR - https://www.biorxiv.org/content/10.64898/2026.09.25.752594v1
AB - 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.
ER -