Abstract
Background: VDAC (Voltage-Dependent Anion selective Channel) is a small family of abundant pore-forming proteins located in the outer mitochondrial membrane. Their role range from the most intuitive, the formation of a hydrophilic conduit through the membrane thanks to its beta-barrel structure, to less understood functions that make them essential actors in the cross-talk between the bioenergetics metabolism and the cytosol components. Due to this localization, VDAC1, in particular, has been reported to be involved in apoptosis, Hexokinase and tubulin binding, and in the Warburg effect. For these reasons, an involvement of VDAC in cancer is considered consequential and a number of compounds have been proposed and used in experimental trials to demonstrate the efficacy of molecules affecting the functions of VDAC.
Objectives: In this work, we thus survey the literature describing drug compounds acting on the cancerous proliferation through VDAC. Three main categories have been assigned: molecules acting on the VDAC-Hexokinase binding, molecules directly inhibiting the VDAC conductance, molecules affecting the expression levels of the VDAC gene. The application of biological peptides for this purpose is also considered.
Conclusion: Since the knowledges about the functional properties of VDAC protein are still insufficient, VDAC as a pharmacological target in the fight against cancer is still a very open, but very promising, field.
Keywords: VDAC, Mitochondrial dysfunction, cancer, apoptosis, hexokinase, warburg effect, outer mitochondrial membrane.
Current Medicinal Chemistry
Title:Anti-Cancer Compounds Targeted to VDAC: Potential and Perspectives
Volume: 24 Issue: 40
Author(s): Simona Reina*Vito De Pinto *
Affiliation:
- Department of Biomedical and Biotechnological Sciences, University of Catania, and National Institute of Biostructures and Biosystems (INBB), Rome, Section of Catania,Italy
- Department of Biomedical and Biotechnological Sciences, University of Catania, and National Institute of Biostructures and Biosystems (INBB), Rome, Section of Catania,Italy
Keywords: VDAC, Mitochondrial dysfunction, cancer, apoptosis, hexokinase, warburg effect, outer mitochondrial membrane.
Abstract: Background: VDAC (Voltage-Dependent Anion selective Channel) is a small family of abundant pore-forming proteins located in the outer mitochondrial membrane. Their role range from the most intuitive, the formation of a hydrophilic conduit through the membrane thanks to its beta-barrel structure, to less understood functions that make them essential actors in the cross-talk between the bioenergetics metabolism and the cytosol components. Due to this localization, VDAC1, in particular, has been reported to be involved in apoptosis, Hexokinase and tubulin binding, and in the Warburg effect. For these reasons, an involvement of VDAC in cancer is considered consequential and a number of compounds have been proposed and used in experimental trials to demonstrate the efficacy of molecules affecting the functions of VDAC.
Objectives: In this work, we thus survey the literature describing drug compounds acting on the cancerous proliferation through VDAC. Three main categories have been assigned: molecules acting on the VDAC-Hexokinase binding, molecules directly inhibiting the VDAC conductance, molecules affecting the expression levels of the VDAC gene. The application of biological peptides for this purpose is also considered.
Conclusion: Since the knowledges about the functional properties of VDAC protein are still insufficient, VDAC as a pharmacological target in the fight against cancer is still a very open, but very promising, field.
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Cite this article as:
Reina Simona *, De Pinto Vito*, Anti-Cancer Compounds Targeted to VDAC: Potential and Perspectives, Current Medicinal Chemistry 2017; 24 (40) . https://dx.doi.org/10.2174/0929867324666170530074039
DOI https://dx.doi.org/10.2174/0929867324666170530074039 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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