Evidence map›Paper›PMID 34959646›Full record

ArticlePharmaceuticals (Basel, Switzerland)2021

Repurposing the Trypanosomatidic GSK Kinetobox for the Inhibition of Parasitic Pteridine and Dihydrofolate Reductases.

Matteo Santucci, Rosaria Luciani, Eleonora Gianquinto, Cecilia Pozzi, Flavio di Pisa, Lucia Dello Iacono, Giacomo Landi, Lorenzo Tagliazucchi, Stefano Mangani, Francesca Spyrakis and 1 more

Open access · goldAbstract read
In one paragraph

Article in Pharmaceuticals (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.9field-weighted citation impact, top 25% 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

5 citing papers in PubMed, 7 citations in OpenAlex.

  1. Review
  2. Article
  3. Deciphering Host-Parasite Interplay inACS infectious diseases · 2024
    Article
  4. Article
  5. 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

11 authors at 3 institutions in 1 country.

Matteo SantucciDepartment of Life Science, University of Modena and Reggio Emilia, Via Campi 103, 41125 Modena, Italy.ORCID 0000-0003-4331-5566
Rosaria LucianiDepartment of Life Science, University of Modena and Reggio Emilia, Via Campi 103, 41125 Modena, Italy.
Eleonora GianquintoDepartment of Drug Science and Technology, University of Turin, Via Giuria 9, 10125 Turin, Italy.
Cecilia PozziDepartment of Biotechnology, Chemistry and Pharmacy-Department of Excellence 2018-2020, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.ORCID 0000-0003-2574-3911
Flavio di PisaDepartment of Biotechnology, Chemistry and Pharmacy-Department of Excellence 2018-2020, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.
Lucia Dello IaconoDepartment of Biotechnology, Chemistry and Pharmacy-Department of Excellence 2018-2020, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.
Giacomo LandiDepartment of Biotechnology, Chemistry and Pharmacy-Department of Excellence 2018-2020, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.
Lorenzo TagliazucchiDepartment of Life Science, University of Modena and Reggio Emilia, Via Campi 103, 41125 Modena, Italy.ORCID 0000-0002-7244-7106
Stefano ManganiDepartment of Biotechnology, Chemistry and Pharmacy-Department of Excellence 2018-2020, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.ORCID 0000-0003-4824-7478
Francesca SpyrakisDepartment of Drug Science and Technology, University of Turin, Via Giuria 9, 10125 Turin, Italy.ORCID 0000-0002-4016-227X
Maria Paola CostiDepartment of Life Science, University of Modena and Reggio Emilia, Via Campi 103, 41125 Modena, Italy.ORCID 0000-0002-0443-5402
University of Siena · ITUniversity of Modena and Reggio Emilia · ITUniversity of Turin · IT

Funding

European Commission 603240
6 · The paper itself

Abstract

Three open-source anti-kinetoplastid chemical boxes derived from a whole-cell phenotypic screening by GlaxoSmithKline (Tres Cantos Anti-Kinetoplastid Screening, TCAKS) were exploited for the discovery of a novel core structure inspiring new treatments of parasitic diseases targeting the trypansosmatidic pteridine reductase 1 (PTR1) and dihydrofolate reductase (DHFR) enzymes. In total, 592 compounds were tested through medium-throughput screening assays. A subset of 14 compounds successfully inhibited the enzyme activity in the low micromolar range of at least one of the enzymes from both

Indexed as

DHFR-TSdrug discoveryGSK KinetoboxLeishmaniasismedium throughput screeningmolecular modellingPTR1trypanosomiasis

Identifiers

PMID34959646
PMCPMC8704748
OpenAlexW3216454242

What Socratic 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 Socratic graph.