Evidence map›Paper›PMID 34927015›Full record

ArticleACS pharmacology & translational science2021

High-Throughput Screening Reveals New Glutaminase Inhibitor Molecules.

Renna K E Costa, Camila T Rodrigues, Jean C H Campos, Luciana S Paradela, Marilia M Dias, Bianca Novaes da Silva, Cyro von Zuben de Valega Negrao, Kaliandra de Almeida Gonçalves, Carolline F R Ascenção, Douglas Adamoski and 8 more

Open access · greenAbstract read
In one paragraph

Article in ACS pharmacology & translational science, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.8field-weighted citation impact, top 33% 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

4 citing papers in PubMed, 12 citations in OpenAlex.

  1. Article
  2. Frontiers in pharmacology · 2024
    Article
  3. Review
  4. Review
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

18 authors at 3 institutions in 1 country.

Renna K E CostaBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.
Camila T RodriguesSao Carlos Institute of Physics (IFSC), University of Sao Paulo (USP), 13563-120 Sao Carlos-SP, Brazil.
Jean C H CamposBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.
Luciana S ParadelaBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.
Marilia M DiasBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.
Bianca Novaes da SilvaBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.
Cyro von Zuben de Valega NegraoBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.
Kaliandra de Almeida GonçalvesBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.
Carolline F R AscençãoBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.
Douglas AdamoskiBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.ORCID https://orcid.org/0000-0001-5062-2586
Gustavo Fernando MercaldiBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.
Alliny C S BastosBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.
Fernanda A H BatistaBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.
Ana Carolina FigueiraBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.ORCID https://orcid.org/0000-0002-7023-8490
Artur T CordeiroBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.ORCID https://orcid.org/0000-0002-5676-2456
Andre L B AmbrosioBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.
Rafael V C GuidoSao Carlos Institute of Physics (IFSC), University of Sao Paulo (USP), 13563-120 Sao Carlos-SP, Brazil.
Sandra M G DiasBrazilian Biosciences National Laboratory (LNBio), Center for Research in Energy and Materials (CNPEM), 13083-100 Campinas-SP, Brazil.ORCID https://orcid.org/0000-0002-1589-7856
Brazilian Center for Research in Energy and Materials · BRUniversidade Estadual de Campinas (UNICAMP) · BRUniversidade de São Paulo · BR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The glutaminase (GLS) enzyme hydrolyzes glutamine into glutamate, an important anaplerotic source for the tricarboxylic acid cycle in rapidly growing cancer cells under the Warburg effect. Glutamine-derived α-ketoglutarate is also an important cofactor of chromatin-modifying enzymes, and through epigenetic changes, it keeps cancer cells in an undifferentiated state. Moreover, glutamate is an important neurotransmitter, and deregulated glutaminase activity in the nervous system underlies several neurological disorders. Given the proven importance of glutaminase for critical diseases, we describe the development of a new coupled enzyme-based fluorescent glutaminase activity assay formatted for 384-well plates for high-throughput screening (HTS) of glutaminase inhibitors. We applied the new methodology to screen a ∼30,000-compound library to search for GLS inhibitors. The HTS assay identified 11 glutaminase inhibitors as hits that were characterized by

Identifiers

PMID34927015
PMCPMC8669713
OpenAlexW3215494099

What OpenQuestion holds

Textmetadata
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.