Evidence map›Paper›PMID 35552392›Full record

ArticleNature communications2022

Molecular basis for inhibiting human glucose transporters by exofacial inhibitors.

Nan Wang, Shuo Zhang, Yafei Yuan, Hanwen Xu, Elisabeth Defossa, Hans Matter, Melissa Besenius, Volker Derdau, Matthias Dreyer, Nis Halland and 6 more

Open access · goldAbstract read
In one paragraph

Article in Nature communications, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.

0numbers the graph read from it
0cells of the map it votes in
21citing papers in PubMed
3.9field-weighted citation impact, top 5% 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

21 citing papers in PubMed, 45 citations in OpenAlex.

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  17. Engineering the MoSAdvanced science (Weinheim, Baden-Wurttemberg, Germany) · 2023
    Article
  18. Review
  19. Article
  20. Profile of Nieng Yan.Proceedings of the National Academy of Sciences of the United States of America · 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

16 authors at 5 institutions in 4 countries.

Nan WangState Key Laboratory of Membrane Biology, Beijing Advanced Innovation Center for Structural Biology, Tsinghua-Peking Joint Center for Life Sciences, School of Life Sciences, Tsinghua University, Beijing, 100084, China.ORCID 0000-0001-6840-5336
Shuo ZhangState Key Laboratory of Membrane Biology, Beijing Advanced Innovation Center for Structural Biology, Tsinghua-Peking Joint Center for Life Sciences, School of Life Sciences, Tsinghua University, Beijing, 100084, China.
Yafei YuanState Key Laboratory of Membrane Biology, Beijing Advanced Innovation Center for Structural Biology, Tsinghua-Peking Joint Center for Life Sciences, School of Life Sciences, Tsinghua University, Beijing, 100084, China.ORCID 0000-0003-0709-5666
Hanwen XuState Key Laboratory of Membrane Biology, Beijing Advanced Innovation Center for Structural Biology, Tsinghua-Peking Joint Center for Life Sciences, School of Life Sciences, Tsinghua University, Beijing, 100084, China.
Elisabeth DefossaSanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
Hans MatterSanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
Melissa BeseniusSanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
Volker DerdauSanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery, Industriepark Höchst, 65926, Frankfurt am Main, Germany.ORCID 0000-0002-3767-643X
Matthias DreyerSanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery, Industriepark Höchst, 65926, Frankfurt am Main, Germany.ORCID 0000-0001-6011-9124
Nis HallandSanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery, Industriepark Höchst, 65926, Frankfurt am Main, Germany.ORCID 0000-0003-1684-9036
Kaihui Hu HeSanofi-Aventis Deutschland GmbH, R&D, CMC Synthetics Early Development Analytics, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
Stefan PetrySanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
Michael PodeschwaSanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
Norbert TennagelsBayer AG, R&D, Pharmaceuticals, TA Endocrinology, Metabolism & Reproductive Health, DIU Exploratory Pathobiology, 42096, Wuppertal, Germany.
Xin JiangState Key Laboratory of Membrane Biology, Beijing Advanced Innovation Center for Structural Biology, Tsinghua-Peking Joint Center for Life Sciences, School of Life Sciences, Tsinghua University, Beijing, 100084, China. xin.jiang@unsw.edu.au.
Nieng YanState Key Laboratory of Membrane Biology, Beijing Advanced Innovation Center for Structural Biology, Tsinghua-Peking Joint Center for Life Sciences, School of Life Sciences, Tsinghua University, Beijing, 100084, China. nyan@princeton.edu.ORCID 0000-0003-4829-7416
Sanofi (Germany) · DECenter for Life Sciences · CNBayer (Germany) · DEPrinceton University · USUNSW Sydney · AU

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Human glucose transporters (GLUTs) are responsible for cellular uptake of hexoses. Elevated expression of GLUTs, particularly GLUT1 and GLUT3, is required to fuel the hyperproliferation of cancer cells, making GLUT inhibitors potential anticancer therapeutics. Meanwhile, GLUT inhibitor-conjugated insulin is being explored to mitigate the hypoglycemia side effect of insulin therapy in type 1 diabetes. Reasoning that exofacial inhibitors of GLUT1/3 may be favored for therapeutic applications, we report here the engineering of a GLUT3 variant, designated GLUT3exo, that can be probed for screening and validating exofacial inhibitors. We identify an exofacial GLUT3 inhibitor SA47 and elucidate its mode of action by a 2.3 Å resolution crystal structure of SA47-bound GLUT3. Our studies serve as a framework for the discovery of GLUTs exofacial inhibitors for therapeutic development.

Indexed as

Glucose Transport Proteins, FacilitativeInsulinGlucoseGlucose Transporter Type 1Glucose Transporter Type 3HumansGlucoseGlucose Transporter Type 1Glucose Transporter Type 3Glucose Transport Proteins, FacilitativeInsulin

Identifiers

PMID35552392
PMCPMC9098912
OpenAlexW4280599136

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.