Evidence map›Paper›PMID 31795096›Full record

ArticleMolecules (Basel, Switzerland)2019

Discovery and Characterisation of Dual Inhibitors of Tryptophan 2,3-Dioxygenase (TDO2) and Indoleamine 2,3-Dioxygenase 1 (IDO1) Using Virtual Screening.

Suat Sari, Petr Tomek, Euphemia Leung, Jóhannes Reynisson

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
1.0field-weighted citation impact, top 27% 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

14 citing papers in PubMed, 29 citations in OpenAlex.

  1. Article
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  11. Pancancer Analysis of RevealedDisease markers · 2022
    Article
  12. Review
  13. Advances in Anticancer Drug Discovery.Molecules (Basel, Switzerland) · 2021
    Article
  14. 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

4 authors at 3 institutions in 3 countries.

Suat SariHacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara 06100, Turkey.ORCID 0000-0002-8248-4218
Petr TomekAuckland Cancer Society Research Centre, University of Auckland, Grafton, 1023 Auckland, New Zealand.ORCID 0000-0002-5490-6540
Euphemia LeungAuckland Cancer Society Research Centre, University of Auckland, Grafton, 1023 Auckland, New Zealand.
Jóhannes ReynissonSchool of Pharmacy and Bioengineering, Keele University, Hornbeam building, Staffordshire ST5 5BG, UK.ORCID 0000-0003-4174-9512
University of Auckland · NZHacettepe University · TRKeele University · GB

Funding

Breast Cancer Foundation New Zealand 1111Cancer Research Trust New Zealand GOT 1717 JGPDF
6 · The paper itself

Abstract

Cancers express tryptophan catabolising enzymes indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO2) to produce immunosuppressive tryptophan metabolites that undermine patients' immune systems, leading to poor disease outcomes. Both enzymes are validated targets for cancer immunotherapy but there is a paucity of potent TDO2 and dual IDO1/TDO2 inhibitors. To identify novel dual IDO1/TDO2 scaffolds, 3D shape similarity and pharmacophore in silico screening was conducted using TDO2 as a model for both systems. The obtained hits were tested in cancer cell lines expressing mainly IDO1 (SKOV3-ovarian), predominantly TDO2 (A172-brain), and both IDO1 and TDO2 (BT549-breast). Three virtual screening hits were confirmed as inhibitors (

Indexed as

Drug DiscoveryAntineoplastic AgentsDrug DevelopmentEnzyme InhibitorsHumansIndoleamine-Pyrrole 2,3,-DioxygenaseLigandsModels, MolecularMolecular StructureStructure-Activity RelationshipTryptophan OxygenaseAntineoplastic AgentsEnzyme InhibitorsIndoleamine-Pyrrole 2,3,-DioxygenaseLigandsTryptophan Oxygenasecancer immunotherapychemical spacehaem-containing dioxygenaseskynurenineligand and pharmacophore-based screeningmolecular modelling

Identifiers

PMID31795096
PMCPMC6930675
OpenAlexW2990158815

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.