Evidence map›Paper›PMID 26332543›Full record

ArticleChemMedChem2015

Salicylketoximes That Target Glucose Transporter 1 Restrict Energy Supply to Lung Cancer Cells.

Carlotta Granchi, Yanrong Qian, Hyang Yeon Lee, Ilaria Paterni, Carolina Pasero, Jessica Iegre, Kathryn E Carlson, Tiziano Tuccinardi, Xiaozhuo Chen, John A Katzenellenbogen and 2 more

Open access · greenAbstract read
In one paragraph

Article in ChemMedChem, 2015. 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
1.1field-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

8 citing papers in PubMed, 20 citations in OpenAlex.

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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

12 authors at 5 institutions in 2 countries.

Carlotta GranchiDipartimento di Farmacia, Università di Pisa, Via Bonanno 33, 56126, Pisa, Italy.
Yanrong QianEdison Biotechnology Institute, Ohio University, the Ridges, Athens, OH, 45701, USA.
Hyang Yeon LeeDepartment of Chemistry, University of Illinois, 600 S. Mathews Avenue, Urbana, IL, 61801, USA.
Ilaria PaterniDipartimento di Farmacia, Università di Pisa, Via Bonanno 33, 56126, Pisa, Italy.
Carolina PaseroDipartimento di Farmacia, Università di Pisa, Via Bonanno 33, 56126, Pisa, Italy.
Jessica IegreDipartimento di Farmacia, Università di Pisa, Via Bonanno 33, 56126, Pisa, Italy.
Kathryn E CarlsonDepartment of Chemistry, University of Illinois, 600 S. Mathews Avenue, Urbana, IL, 61801, USA.
Tiziano TuccinardiDipartimento di Farmacia, Università di Pisa, Via Bonanno 33, 56126, Pisa, Italy.
Xiaozhuo ChenEdison Biotechnology Institute, Ohio University, the Ridges, Athens, OH, 45701, USA.
John A KatzenellenbogenDepartment of Chemistry, University of Illinois, 600 S. Mathews Avenue, Urbana, IL, 61801, USA.
Paul J HergenrotherDepartment of Chemistry, University of Illinois, 600 S. Mathews Avenue, Urbana, IL, 61801, USA.
Filippo MinutoloDipartimento di Farmacia, Università di Pisa, Via Bonanno 33, 56126, Pisa, Italy. filippo.minutolo@farm.unipi.it.
University of Pisa · ITUniversity of Illinois Urbana-Champaign · USBiotechnology Institute · USOhio University · USUrbana University · US

Funding

MOLECULAR PROBES FOR STEROID RECEPTORSR37DK015556 · NIDDK · UNIVERSITY OF ILLINOIS URBANA-CHAMPAIGN · PI KATZENELLENBOGEN, JOHN A. · 1987 to 2012
$4.4M
Design, Synthesis, and Evaluation of Lactate Dehydrogenase InhibitorsR01GM098453 · NIGMS · UNIVERSITY OF ILLINOIS AT URBANA-CHAMPAIGN · PI HERGENROTHER, PAUL · 2012 to 2015
$1.8M
Novel Ligands and Mechanisms to Achieve Selective Nuclear Receptor ActivityR01DK015556 · NIDDK · UNIVERSITY OF ILLINOIS URBANA-CHAMPAIGN · PI KATZENELLENBOGEN, JOHN A. · 1986 to 2016
$1.6M
NIDDK NIH HHS R01 DK015556NIDDK NIH HHS R37 DK015556NIGMS NIH HHS R01 GM098453PHS HHS R01K015556PHS HHS R01M098453
6 · The paper itself

Abstract

The glucose transporter GLUT1 is frequently overexpressed in most tumor tissues because rapidly proliferating cancer cells rely primarily on glycolysis, a low-efficiency metabolic pathway that necessitates a very high rate of glucose consumption. Because blocking GLUT1 is a promising anticancer strategy, we developed a novel class of GLUT1 inhibitors based on the 4-aryl-substituted salicylketoxime scaffold. Some of these compounds are efficient inhibitors of glucose uptake in lung cancer cells and have a notable antiproliferative effect. In contrast to their 5-aryl-substituted regioisomers, the newly synthesized compounds reported herein do not display significant binding to the estrogen receptors. The inhibition of glucose uptake in cancer cells by these compounds was further observed by fluorescence microscopy imaging using a fluorescent analogue of glucose. Therefore, blocking the ability of tumor cells to take up glucose by means of these small molecules, or by further optimized derivatives, may be a successful approach in the development of novel anticancer drugs.

Indexed as

AnimalsAntineoplastic AgentsCell Line, TumorCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorEnergy MetabolismGlucose Transporter Type 1HumansLung NeoplasmsMiceMolecular StructureNeoplasms, ExperimentalOximesStructure-Activity RelationshipAntineoplastic AgentsGlucose Transporter Type 1OximesSLC2A1 protein, humancancer metabolismGLUT1glycolysisoximesWarburg effect

Identifiers

PMID26332543
PMCPMC4743644
OpenAlexW2160865264

What OpenQuestion holds

Textmetadata
LicenceTDM
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.