Evidence map›Paper›PMID 33565680›Full record

ArticleAngewandte Chemie (International ed. in English)2021

Cell-Based Identification of New IDO1 Modulator Chemotypes.

Elisabeth Hennes, Philipp Lampe, Lara Dötsch, Nora Bruning, Lisa-Marie Pulvermacher, Sonja Sievers, Slava Ziegler, Herbert Waldmann

Open access · hybridAbstract read
In one paragraph

Article in Angewandte Chemie (International ed. in English), 2021. 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
0.9field-weighted citation impact, top 34% 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

8 citing papers in PubMed, 18 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Article
  5. Article
  6. Review
  7. Identification of a Novel Pseudo-Natural Product Type IV IDO1 Inhibitor Chemotype.Angewandte Chemie (International ed. in English) · 2022
    Article
  8. Cell-Based Identification of New IDO1 Modulator Chemotypes.Angewandte Chemie (International ed. in English) · 2021
    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

8 authors at 2 institutions in 1 country.

Elisabeth HennesDepartment of Chemical Biology, Max Planck Institute of Molecular Physiology, Otto-Hahn-Str. 11, 44227, Dortmund, Germany.
Philipp LampeCompound Management and Screening Center, Otto-Hahn-Str.11, 44227, Dortmund, Germany.
Lara DötschDepartment of Chemical Biology, Max Planck Institute of Molecular Physiology, Otto-Hahn-Str. 11, 44227, Dortmund, Germany.
Nora BruningDepartment of Chemical Biology, Technical University of Dortmund, Otto-Hahn-Strasse 6, 44227, Dortmund, Germany.
Lisa-Marie PulvermacherDepartment of Chemical Biology, Technical University of Dortmund, Otto-Hahn-Strasse 6, 44227, Dortmund, Germany.
Sonja SieversCompound Management and Screening Center, Otto-Hahn-Str.11, 44227, Dortmund, Germany.ORCID 0000-0003-0854-4507
Slava ZieglerDepartment of Chemical Biology, Max Planck Institute of Molecular Physiology, Otto-Hahn-Str. 11, 44227, Dortmund, Germany.ORCID 0000-0003-4398-7741
Herbert WaldmannDepartment of Chemical Biology, Max Planck Institute of Molecular Physiology, Otto-Hahn-Str. 11, 44227, Dortmund, Germany.ORCID 0000-0002-9606-7247
TU Dortmund University · DEMax Planck Institute of Molecular Physiology · DE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The immunoregulatory enzyme indoleamine-2,3-dioxygenase (IDO1) strengthens cancer immune escape, and inhibition of IDO1 by means of new chemotypes and mechanisms of action is considered a promising opportunity for IDO1 inhibitor discovery. IDO1 is a cofactor-binding, redox-sensitive protein, which calls for monitoring of IDO1 activity in its native cellular environment. We developed a new, robust fluorescence-based assay amenable to high throughput, which detects kynurenine in cells. Screening of a ca. 150 000-member compound library discovered unprecedented, potent IDO1 modulators with different mechanisms of action, including direct IDO1 inhibitors, regulators of IDO1 expression, and inhibitors of heme synthesis. Three IDO1-modulator chemotypes were identified that bind to apo-IDO1 and compete with the heme cofactor. Our new cell-based technology opens up novel opportunities for medicinal chemistry programs in immuno-oncology.

Indexed as

Cell Line, TumorCoumarinsEnzyme InhibitorsFluorescent DyesHumansIndoleamine-Pyrrole 2,3,-DioxygenaseKynurenineMolecular StructurecoumarinCoumarinsEnzyme InhibitorsFluorescent DyesIDO1 protein, humanIndoleamine-Pyrrole 2,3,-DioxygenaseKynureninecancerfluorescenceheme proteinshigh throughput screeningimmunology

Identifiers

PMID33565680
PMCPMC8252559
OpenAlexW3127555312

What OpenQuestion holds

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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.