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Peer-reviewedCC BY 4.0eLife

A membrane-disruptive action of VBIT-4 challenges its role as a widely used VDAC1 oligomerization inhibitor

  • Varun Ravishankar
  • Luís Borges-Araújo
  • Megha Rajendran
  • Elodie Lafargue
  • Deborah Byrne
  • Nicolas Buzhinsky
  • Mya S Wolfe
  • Wendy Fitzgerald
  • Nina A Bautista
  • Bethel G Beyene
  • Motahareh G Larimi
  • Jean-Pierre Duneau
5 more authors
  • James Sturgis
  • Sergey M Bezrukov
  • Ignacio Casuso
  • Tatiana K Rostovtseva
  • Lucie Bergdoll
Open at sourcePDFDOICite

Abstract

This work provides a reassessment of VBIT-4, a compound previously proposed to inhibit oligomerization of the crucial protein known as the mitochondrial voltage-dependent anion channel. Combining complementary experimental approaches with molecular dynamics simulations, the authors provide compelling evidence that VBIT-4 primarily disrupts lipid membranes and induces channel-independent cytotoxicity. The study has fundamental implications for interpreting previous work using VBIT-4 as a probe of channel function and highlights the need to consider membranedisruptive effects when evaluating drug mechanisms.

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Cite

BibTeXRIS
BibTeX
@article{ravishankar2026membranedisruptive,
  title = {{A membrane-disruptive action of VBIT-4 challenges its role as a widely used VDAC1 oligomerization inhibitor}},
  author = {Varun Ravishankar and Luís Borges-Araújo and Megha Rajendran and Elodie Lafargue and Deborah Byrne and Nicolas Buzhinsky and Mya S Wolfe and Wendy Fitzgerald and Nina A Bautista and Bethel G Beyene and Motahareh G Larimi and Jean-Pierre Duneau and James Sturgis and Sergey M Bezrukov and Ignacio Casuso and Tatiana K Rostovtseva and Lucie Bergdoll},
  journal = {eLife},
  year = {2026},
  month = oct,
  doi = {10.7554/elife.111980},
  url = {https://hal.science/hal-05793971v1},
  note = {CC BY 4.0},
}
RIS
TY  - JOUR
TI  - A membrane-disruptive action of VBIT-4 challenges its role as a widely used VDAC1 oligomerization inhibitor
AU  - Varun Ravishankar
AU  - Luís Borges-Araújo
AU  - Megha Rajendran
AU  - Elodie Lafargue
AU  - Deborah Byrne
AU  - Nicolas Buzhinsky
AU  - Mya S Wolfe
AU  - Wendy Fitzgerald
AU  - Nina A Bautista
AU  - Bethel G Beyene
AU  - Motahareh G Larimi
AU  - Jean-Pierre Duneau
AU  - James Sturgis
AU  - Sergey M Bezrukov
AU  - Ignacio Casuso
AU  - Tatiana K Rostovtseva
AU  - Lucie Bergdoll
PY  - 2026
DA  - 2026/10/09
JO  - eLife
DO  - 10.7554/elife.111980
UR  - https://hal.science/hal-05793971v1
AB  - This work provides a reassessment of VBIT-4, a compound previously proposed to inhibit oligomerization of the crucial protein known as the mitochondrial voltage-dependent anion channel. Combining complementary experimental approaches with molecular dynamics simulations, the authors provide compelling evidence that VBIT-4 primarily disrupts lipid membranes and induces channel-independent cytotoxicity. The study has fundamental implications for interpreting previous work using VBIT-4 as a probe of channel function and highlights the need to consider membranedisruptive effects when evaluating drug mechanisms.
SN  - 2050-084X
ER  -