Evidence map›Paper›PMID 31469221›Full record

ArticleAngewandte Chemie (International ed. in English)2019

Synthesis of Indomorphan Pseudo-Natural Product Inhibitors of Glucose Transporters GLUT-1 and -3.

Javier Ceballos, Melanie Schwalfenberg, George Karageorgis, Elena S Reckzeh, Sonja Sievers, Claude Ostermann, Axel Pahl, Magnus Sellstedt, Jessica Nowacki, Marjorie A Carnero Corrales and 10 more

Open access · hybridAbstract read
In one paragraph

Article in Angewandte Chemie (International ed. in English), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.

0numbers the graph read from it
0cells of the map it votes in
44citing papers in PubMed
4.4field-weighted citation impact, top 4% 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

44 citing papers in PubMed, 98 citations in OpenAlex.

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  20. Identification of a Novel Pseudo-Natural Product Type IV IDO1 Inhibitor Chemotype.Angewandte Chemie (International ed. in English) · 2022
    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

20 authors at 5 institutions in 6 countries.

Javier CeballosDepartment of Chemical Biology, Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
Melanie SchwalfenbergDepartment of Chemical Biology, Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
George KarageorgisDepartment of Chemical Biology, Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
Elena S ReckzehDepartment of Chemical Biology, Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
Sonja SieversCompound Management and Screening Center, Dortmund, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
Claude OstermannCompound Management and Screening Center, Dortmund, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
Axel PahlCompound Management and Screening Center, Dortmund, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
Magnus SellstedtDepartment of Chemistry, Umeå University, 901 87, Umeå, Sweden.
Jessica NowackiDepartment of Chemical Biology, Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
Marjorie A Carnero CorralesDepartment of Chemical Biology, Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
Julian WilkeDepartment of Chemical Biology, Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
Luca LaraiaDepartment of Chemical Biology, Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
Kirsten TschapaldaDepartment of Chemical Biology, Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
Malte MetzDepartment of Chemical Biology, Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
Dominik A SehrDepartment of Molecular Cell Biology, Institute of Biochemistry and Pathobiochemistry, Ruhr University Bochum, 44801, Bochum, Germany.
Silke BrandDepartment of Chemical Biology, Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
Konstanze WinklhoferDepartment of Molecular Cell Biology, Institute of Biochemistry and Pathobiochemistry, Ruhr University Bochum, 44801, Bochum, Germany.
Petra JanningDepartment of Chemical Biology, Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
Slava ZieglerDepartment of Chemical Biology, Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
Herbert WaldmannDepartment of Chemical Biology, Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.ORCID 0000-0002-9606-7247
Max Planck Institute of Molecular Physiology · DETU Dortmund University · DERuhr University Bochum · DEUniversity Hospital of Umeå · SEUniversity of Leeds · GB

Funding

Alexander von Humboldt-StiftungFonds der Chemischen IndustrieFP7 Ideas: European Research Council 268309Swedish Research Council 350-2012-6611Swiss National Science Foundation
6 · The paper itself

Abstract

Bioactive compound design based on natural product (NP) structure may be limited because of partial coverage of NP-like chemical space and biological target space. These limitations can be overcome by combining NP-centered strategies with fragment-based compound design through combination of NP-derived fragments to afford structurally unprecedented "pseudo-natural products" (pseudo-NPs). The design, synthesis, and biological evaluation of a collection of indomorphan pseudo-NPs that combine biosynthetically unrelated indole- and morphan-alkaloid fragments are described. Indomorphane derivative Glupin was identified as a potent inhibitor of glucose uptake by selectively targeting and upregulating glucose transporters GLUT-1 and GLUT-3. Glupin suppresses glycolysis, reduces the levels of glucose-derived metabolites, and attenuates the growth of various cancer cell lines. Our findings underscore the importance of dual GLUT-1 and GLUT-3 inhibition to efficiently suppress tumor cell growth and the cellular rescue mechanism, which counteracts glucose scarcity.

Indexed as

Cell ProliferationBiological ProductsBiological TransportCell CycleGlucoseGlucose Transporter Type 1Glucose Transporter Type 3GlycolysisHumansMorphinansNeoplasmsTumor Cells, CulturedBiological ProductsGlucoseGlucose Transporter Type 1Glucose Transporter Type 3MorphinansSLC2A1 protein, humanSLC2A3 protein, humanantitumor agentsglucose transportersinhibitorsnatural productspseudo-natural products

Identifiers

PMID31469221
PMCPMC6900016
OpenAlexW2970488722

What OpenQuestion holds

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Registered trials

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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.