A high-throughput screening dataset of small-molecule inhibitors across human DNA glycosylases
Year: 2026
Type: preprint
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. Abstract Figure
Authors: Alice Eddershaw, Bjørn Dalhus, Opher Gileadi, Susanne Gräslund, İrşil Güneş, Thomas Helleday, Kang-Cheng Liu, Olga Loseva, Vu To Nakstad, Hilde Loge Nilsen, Nicola P. Montaldo, Karen Nierlin, Carina Norström, Natálie Rudolfová, Kristine Sletta, Michael Sundström, Rahul Upadhyay, Barbara van Loon, Edvard Wigren, Elisée Wiita, Ane Marit Wågbø, Kaixin Zhou, Evert J. Homan, Torkild Visnes, Maurice Michel
Language: English
Topic: DNA Repair Mechanisms
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: green
OpenAlex ID: W7214649994