Evidence map›Paper›PMID 38569218›Full record

ArticleAdvanced science (Weinheim, Baden-Wurttemberg, Germany)2024

Discovery of a Novel Pseudo-Natural Product Aurora Kinase Inhibitor Chemotype through Morphological Profiling.

Lin Wang, Furkan Yilmaz, Okan Yildirim, Beate Schölermann, Sukdev Bag, Luca Greiner, Axel Pahl, Sonja Sievers, Rebecca Scheel, Carsten Strohmann and 5 more

Abstract read
In one paragraph

Article in Advanced science (Weinheim, Baden-Wurttemberg, Germany), 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
–field-weighted citation impact
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

8 citing papers in PubMed.

  1. JACS Au · 2026
    Article
  2. Article
  3. Review
  4. An Indole Dearomatization Strategy for the Synthesis of Pseudo-Natural Products.Chembiochem : a European journal of chemical biology · 2025
    Article
  5. Article
  6. Article
  7. Article
  8. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

15 authors.

Lin WangDepartment of Chemical Biology, Max Planck Institute of Molecular Physiology, 44227, Dortmund, Germany.
Furkan YilmazDepartment of Chemical Biology, Max Planck Institute of Molecular Physiology, 44227, Dortmund, Germany.
Okan YildirimDepartment of Chemical Biology, Max Planck Institute of Molecular Physiology, 44227, Dortmund, Germany.
Beate SchölermannDepartment of Chemical Biology, Max Planck Institute of Molecular Physiology, 44227, Dortmund, Germany.
Sukdev BagDepartment of Chemical Biology, Max Planck Institute of Molecular Physiology, 44227, Dortmund, Germany.
Luca GreinerDepartment of Chemical Biology, Max Planck Institute of Molecular Physiology, 44227, Dortmund, Germany.
Axel PahlDepartment of Chemical Biology, Max Planck Institute of Molecular Physiology, 44227, Dortmund, Germany.ORCID 0000-0003-2068-7543
Sonja SieversDepartment of Chemical Biology, Max Planck Institute of Molecular Physiology, 44227, Dortmund, Germany.ORCID 0000-0003-0854-4507
Rebecca ScheelFaculty of Chemistry and Inorganic Chemistry, TU Dortmund University, 44227, Dortmund, Germany.
Carsten StrohmannFaculty of Chemistry and Inorganic Chemistry, TU Dortmund University, 44227, Dortmund, Germany.ORCID 0000-0002-4787-2135
Christopher SquireSchool of Biological Sciences, University of Auckland, 1142, Auckland, New Zealand.
Daniel J FoleySchool of Physical and Chemical Sciences, University of Canterbury, 8041, Christchurch, New Zealand.
Slava ZieglerDepartment of Chemical Biology, Max Planck Institute of Molecular Physiology, 44227, Dortmund, Germany.ORCID 0000-0003-4398-7741
Michael GrigalunasDepartment of Chemical Biology, Max Planck Institute of Molecular Physiology, 44227, Dortmund, Germany.ORCID 0000-0003-0419-8168
Herbert WaldmannDepartment of Chemical Biology, Max Planck Institute of Molecular Physiology, 44227, Dortmund, Germany.ORCID 0000-0002-9606-7247

Funding

European Union EFRE-0200481Innovative Medicines Initiative 115489Seventh Framework Programme FP7/2007-2013
6 · The paper itself

Abstract

The pseudo-natural product (pseudo-NP) concept aims to combine NP fragments in arrangements that are not accessible through known biosynthetic pathways. The resulting compounds retain the biological relevance of NPs but are not yet linked to bioactivities and may therefore be best evaluated by unbiased screening methods resulting in the identification of unexpected or unprecedented bioactivities. Herein, various NP fragments are combined with a tricyclic core connectivity via interrupted Fischer indole and indole dearomatization reactions to provide a collection of highly three-dimensional pseudo-NPs. Target hypothesis generation by morphological profiling via the cell painting assay guides the identification of an unprecedented chemotype for Aurora kinase inhibition with both its relatively highly 3D structure and its physicochemical properties being very different from known inhibitors. Biochemical and cell biological characterization indicate that the phenotype identified by the cell painting assay corresponds to the inhibition of Aurora kinase B.

Indexed as

Biological ProductsProtein Kinase InhibitorsAurora Kinase BAurora KinasesDrug DiscoveryHumansAurora Kinase BAurora KinasesBiological ProductsProtein Kinase InhibitorsAurora kinase inhibitorindole dearomatizationinterrupted fischer indolemorphological profilingpseudo‐natural products

Identifiers

PMID38569218
PMCPMC11151026

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

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.