Article in RSC medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 2 papers.
0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.3field-weighted citation impact, top 44% of its field
1 · What the graph read from it
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
2 · The registry
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
3 · Its place in the literature
Who cites it
2 citing papers in PubMed, 4 citations in OpenAlex.
Shubhendu PaleiDepartment of Chemistry and Chemical Biology, TU Dortmund University and, Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) Otto-Hahn Str. 4a 44227 Dortmund Germany guido.clever@tu-dortmund.de daniel.rauh@tu-dortmund.de daniel.summerer@tu-dortmund.de.
Jörn WeisnerDepartment of Chemistry and Chemical Biology, TU Dortmund University and, Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) Otto-Hahn Str. 4a 44227 Dortmund Germany guido.clever@tu-dortmund.de daniel.rauh@tu-dortmund.de daniel.summerer@tu-dortmund.de.ORCID https://orcid.org/0000-0002-6103-7371
Melina VogtDepartment of Chemistry and Chemical Biology, TU Dortmund University and, Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) Otto-Hahn Str. 4a 44227 Dortmund Germany guido.clever@tu-dortmund.de daniel.rauh@tu-dortmund.de daniel.summerer@tu-dortmund.de.
Rajesh GontlaDepartment of Chemistry and Chemical Biology, TU Dortmund University and, Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) Otto-Hahn Str. 4a 44227 Dortmund Germany guido.clever@tu-dortmund.de daniel.rauh@tu-dortmund.de daniel.summerer@tu-dortmund.de.
Benjamin BuchmullerDepartment of Chemistry and Chemical Biology, TU Dortmund University and, Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) Otto-Hahn Str. 4a 44227 Dortmund Germany guido.clever@tu-dortmund.de daniel.rauh@tu-dortmund.de daniel.summerer@tu-dortmund.de.ORCID https://orcid.org/0000-0002-4915-5949
Christiane EhrtDepartment of Chemistry and Chemical Biology, TU Dortmund University and, Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) Otto-Hahn Str. 4a 44227 Dortmund Germany guido.clever@tu-dortmund.de daniel.rauh@tu-dortmund.de daniel.summerer@tu-dortmund.de.
Tobias GrabeDepartment of Chemistry and Chemical Biology, TU Dortmund University and, Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) Otto-Hahn Str. 4a 44227 Dortmund Germany guido.clever@tu-dortmund.de daniel.rauh@tu-dortmund.de daniel.summerer@tu-dortmund.de.
Silke KleinböltingDepartment of Chemistry and Chemical Biology, TU Dortmund University and, Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) Otto-Hahn Str. 4a 44227 Dortmund Germany guido.clever@tu-dortmund.de daniel.rauh@tu-dortmund.de daniel.summerer@tu-dortmund.de.
Matthias MüllerDepartment of Chemistry and Chemical Biology, TU Dortmund University and, Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) Otto-Hahn Str. 4a 44227 Dortmund Germany guido.clever@tu-dortmund.de daniel.rauh@tu-dortmund.de daniel.summerer@tu-dortmund.de.ORCID https://orcid.org/0000-0002-1529-8933
Guido H CleverDepartment of Chemistry and Chemical Biology, TU Dortmund University and, Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) Otto-Hahn Str. 4a 44227 Dortmund Germany guido.clever@tu-dortmund.de daniel.rauh@tu-dortmund.de daniel.summerer@tu-dortmund.de.ORCID https://orcid.org/0000-0001-8458-3060
Daniel RauhDepartment of Chemistry and Chemical Biology, TU Dortmund University and, Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) Otto-Hahn Str. 4a 44227 Dortmund Germany guido.clever@tu-dortmund.de daniel.rauh@tu-dortmund.de daniel.summerer@tu-dortmund.de.ORCID https://orcid.org/0000-0002-1970-7642
Daniel SummererDepartment of Chemistry and Chemical Biology, TU Dortmund University and, Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW) Otto-Hahn Str. 4a 44227 Dortmund Germany guido.clever@tu-dortmund.de daniel.rauh@tu-dortmund.de daniel.summerer@tu-dortmund.de.ORCID https://orcid.org/0000-0002-3019-7241
TU Dortmund University · DE
Funding
No grant is acknowledged in the PubMed record.
6 · The paper itself
Abstract
Ten-eleven translocation dioxygenases (TETs) are the erasers of 5-methylcytosine (mC), the central epigenetic regulator of mammalian DNA. TETs convert mC to three oxidized derivatives with unique physicochemical properties and inherent regulatory potential, and it initializes active demethylation by the base excision repair pathway. Potent small molecule inhibitors would be useful tools to study TET functions by conditional control. To facilitate the discovery of such tools, we here report a high-throughput screening pipeline and its application to screen and validate 31.5k compounds for inhibition of TET2. Using a homogenous fluorescence assay, we discover a novel quinoline-based scaffold that we further validate with an orthogonal semi-high throughput MALDI-MS assay for direct monitoring of substrate turnover. Structure-activity relationship (SAR) studies involving >20 derivatives of this scaffold led to the identification of optimized inhibitors, and together with computational studies suggested a plausible model for its mode of action.
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.
A high-throughput effector screen identifies a novel small molecule scaffold for inhibition of ten-eleven translocation dioxygenase 2. · full record | OpenQuestion