Hexokinase-I directly binds to a charged membrane-buried glutamate of mitochondrial VDAC1 and VDAC2

Abstract Binding of hexokinase HKI to mitochondrial voltage-dependent anion channels (VDACs) has far-reaching physiological implications. However, the structural basis of this interaction is unclear. Combining computer simulations with experiments in cells, we here show that complex assembly relies...

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Main Authors: Sebastian Bieker, Michael Timme, Nils Woge, Dina G. Hassan, Chelsea M. Brown, Siewert J. Marrink, Manuel N. Melo, Joost C. M. Holthuis
Format: Article
Language:English
Published: Nature Portfolio 2025-02-01
Series:Communications Biology
Online Access:https://doi.org/10.1038/s42003-025-07551-9
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author Sebastian Bieker
Michael Timme
Nils Woge
Dina G. Hassan
Chelsea M. Brown
Siewert J. Marrink
Manuel N. Melo
Joost C. M. Holthuis
author_facet Sebastian Bieker
Michael Timme
Nils Woge
Dina G. Hassan
Chelsea M. Brown
Siewert J. Marrink
Manuel N. Melo
Joost C. M. Holthuis
author_sort Sebastian Bieker
collection DOAJ
description Abstract Binding of hexokinase HKI to mitochondrial voltage-dependent anion channels (VDACs) has far-reaching physiological implications. However, the structural basis of this interaction is unclear. Combining computer simulations with experiments in cells, we here show that complex assembly relies on intimate contacts between the N-terminal α-helix of HKI and a charged membrane-buried glutamate on the outer wall of VDAC1 and VDAC2. Protonation of this residue blocks complex formation in silico while acidification of the cytosol causes a reversable release of HKI from mitochondria. Membrane insertion of HKI occurs adjacent to the bilayer-facing glutamate where a pair of polar channel residues mediates a marked thinning of the cytosolic leaflet. Disrupting the membrane thinning capacity of VDAC1 dramatically impairs its ability to bind HKI in silico and in cells. Our data reveal key topological and mechanistic insights into HKI-VDAC complex assembly that may benefit the development of therapeutics to counter pathogenic imbalances in this process.
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spelling doaj-art-e5622aec85b64030840269ad066dc8c72025-08-20T03:01:00ZengNature PortfolioCommunications Biology2399-36422025-02-018111710.1038/s42003-025-07551-9Hexokinase-I directly binds to a charged membrane-buried glutamate of mitochondrial VDAC1 and VDAC2Sebastian Bieker0Michael Timme1Nils Woge2Dina G. Hassan3Chelsea M. Brown4Siewert J. Marrink5Manuel N. Melo6Joost C. M. Holthuis7Molecular Cell Biology Division, Department of Biology/Chemistry, University of OsnabrückMolecular Cell Biology Division, Department of Biology/Chemistry, University of OsnabrückMolecular Cell Biology Division, Department of Biology/Chemistry, University of OsnabrückMolecular Cell Biology Division, Department of Biology/Chemistry, University of OsnabrückGroningen Biomolecular Sciences and Biotechnology Institute, University of Groningen, Nijenborgh 7Groningen Biomolecular Sciences and Biotechnology Institute, University of Groningen, Nijenborgh 7Instituto de Tecnologia Química e Biológica António Xavier, Universidade Nova de Lisboa, Av. da RepúblicaMolecular Cell Biology Division, Department of Biology/Chemistry, University of OsnabrückAbstract Binding of hexokinase HKI to mitochondrial voltage-dependent anion channels (VDACs) has far-reaching physiological implications. However, the structural basis of this interaction is unclear. Combining computer simulations with experiments in cells, we here show that complex assembly relies on intimate contacts between the N-terminal α-helix of HKI and a charged membrane-buried glutamate on the outer wall of VDAC1 and VDAC2. Protonation of this residue blocks complex formation in silico while acidification of the cytosol causes a reversable release of HKI from mitochondria. Membrane insertion of HKI occurs adjacent to the bilayer-facing glutamate where a pair of polar channel residues mediates a marked thinning of the cytosolic leaflet. Disrupting the membrane thinning capacity of VDAC1 dramatically impairs its ability to bind HKI in silico and in cells. Our data reveal key topological and mechanistic insights into HKI-VDAC complex assembly that may benefit the development of therapeutics to counter pathogenic imbalances in this process.https://doi.org/10.1038/s42003-025-07551-9
spellingShingle Sebastian Bieker
Michael Timme
Nils Woge
Dina G. Hassan
Chelsea M. Brown
Siewert J. Marrink
Manuel N. Melo
Joost C. M. Holthuis
Hexokinase-I directly binds to a charged membrane-buried glutamate of mitochondrial VDAC1 and VDAC2
Communications Biology
title Hexokinase-I directly binds to a charged membrane-buried glutamate of mitochondrial VDAC1 and VDAC2
title_full Hexokinase-I directly binds to a charged membrane-buried glutamate of mitochondrial VDAC1 and VDAC2
title_fullStr Hexokinase-I directly binds to a charged membrane-buried glutamate of mitochondrial VDAC1 and VDAC2
title_full_unstemmed Hexokinase-I directly binds to a charged membrane-buried glutamate of mitochondrial VDAC1 and VDAC2
title_short Hexokinase-I directly binds to a charged membrane-buried glutamate of mitochondrial VDAC1 and VDAC2
title_sort hexokinase i directly binds to a charged membrane buried glutamate of mitochondrial vdac1 and vdac2
url https://doi.org/10.1038/s42003-025-07551-9
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