In silico construction of HK2-VDAC1 complex and investigating the HK2 binding-induced molecular gating mechanism of VDAC1

Mitochondrion. 2016 Sep:30:222-8. doi: 10.1016/j.mito.2016.08.009. Epub 2016 Aug 17.

Abstract

Hexokinase 2 (HK2) binds to Voltage-Dependent Anion Channel 1 (VDAC1) on mitochondrial outer membrane (MOM) to facilitate a preferential access of ATP to HK2 for glycolysis, in order to maintain a constant energy source for cell proliferation in cancer especially. While previous studies have discovered that the VDAC1 N-terminal helix is responsible for regulating molecules from within mitochondria to cytoplasm, the molecular mechanism of how HK2 is able to regulate the ATP access remains elusive. We hereby propose a model for the HK2-VDAC1 association. The model is then subjected to molecular dynamics (MD) simulations, where we probe the effect of HK2 binding on the mobility of the VDAC1 N-terminal helix. Results from the simulations show that HK2 binding restricts the movement of the VDAC1 N-terminal helix. As a result, VDAC1 is kept in the open state most of the time and probably allows a constant supply of ATP to HK2 for glycolysis.

Keywords: Glycolysis; Hexokinase 2; Mitochondrion; Molecular gate; Voltage-Dependent Anion Channel 1.

MeSH terms

  • Adenosine Triphosphate / metabolism*
  • Hexokinase / chemistry*
  • Hexokinase / metabolism*
  • Models, Biological
  • Models, Molecular
  • Molecular Dynamics Simulation
  • Protein Binding
  • Voltage-Dependent Anion Channel 1 / chemistry*
  • Voltage-Dependent Anion Channel 1 / metabolism*

Substances

  • VDAC1 protein, human
  • Adenosine Triphosphate
  • Voltage-Dependent Anion Channel 1
  • HK2 protein, human
  • Hexokinase