Nature Communications (May 2022)
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,
- Kaihui Hu He,
- Stefan Petry,
- Michael Podeschwa,
- Norbert Tennagels,
- Xin Jiang,
- Nieng Yan
Affiliations
- Nan Wang
- State 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
- Shuo Zhang
- State 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
- Yafei Yuan
- State 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
- Hanwen Xu
- State 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
- Elisabeth Defossa
- Sanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery
- Hans Matter
- Sanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery
- Melissa Besenius
- Sanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery
- Volker Derdau
- Sanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery
- Matthias Dreyer
- Sanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery
- Nis Halland
- Sanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery
- Kaihui Hu He
- Sanofi-Aventis Deutschland GmbH, R&D, CMC Synthetics Early Development Analytics
- Stefan Petry
- Sanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery
- Michael Podeschwa
- Sanofi-Aventis Deutschland GmbH, R&D, Integrated Drug Discovery
- Norbert Tennagels
- Bayer AG, R&D, Pharmaceuticals, TA Endocrinology, Metabolism & Reproductive Health, DIU Exploratory Pathobiology
- Xin Jiang
- State 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
- Nieng Yan
- State 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
- DOI
- https://doi.org/10.1038/s41467-022-30326-3
- Journal volume & issue
-
Vol. 13,
no. 1
pp. 1 – 10
Abstract
Human glucose transporters (GLUTs), particularly GLUT1 and GLUT3, are potential anticancer therapy targets. Here, Nan Wang et al. use an engineered GLUT 3 variant to identify an exofacial GLUT3 inhibitor, SA47, and elucidate the drug’s inhibitory mechanism.