Membrane-lipid therapy: A historical perspective of membrane-targeted therapies - From lipid bilayer structure to the pathophysiological regulation of cells

Biochim Biophys Acta Biomembr. 2017 Sep;1859(9 Pt B):1493-1506. doi: 10.1016/j.bbamem.2017.05.017. Epub 2017 Jun 1.

Abstract

Our current understanding of membrane lipid composition, structure and functions has led to the investigation of their role in cell signaling, both in healthy and pathological cells. As a consequence, therapies based on the regulation of membrane lipid composition and structure have been recently developed. This novel field, known as Membrane Lipid Therapy, is growing and evolving rapidly, providing treatments that are now in use or that are being studied for their application to oncological disorders, Alzheimer's disease, spinal cord injury, stroke, diabetes, obesity, and neuropathic pain. This field has arisen from relevant discoveries on the behavior of membranes in recent decades, and it paves the way to adopt new approaches in modern pharmacology and nutrition. This innovative area will promote further investigation into membranes and the development of new therapies with molecules that target the cell membrane. Due to the prominent roles of membranes in the cells' physiology and the paucity of therapeutic approaches based on the regulation of the lipids they contain, it is expected that membrane lipid therapy will provide new treatments for numerous pathologies. The first on-purpose rationally designed molecule in this field, minerval, is currently being tested in clinical trials and it is expected to enter the market around 2020. However, it seems feasible that during the next few decades other membrane regulators will also be marketed for the treatment of human pathologies. This article is part of a Special Issue entitled: Membrane Lipid Therapy: Drugs Targeting Biomembranes edited by Pablo V. Escribá.

Keywords: Lipids in Alzheimer's disease drug discovery; Lipids in cancer drug discovery; Lipids in pathophysiology; Membrane lipid composition and structure; Membrane-targeting therapies; Peripheral membrane protein localization and activity.

Publication types

  • Editorial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Membrane / drug effects*
  • Cell Membrane / physiology
  • Drug Design
  • Humans
  • Inflammation / drug therapy
  • Lipid Bilayers / chemistry*
  • Membrane Lipids / chemistry*
  • Metabolic Diseases / drug therapy
  • Neoplasms / drug therapy
  • Neurodegenerative Diseases / drug therapy

Substances

  • Lipid Bilayers
  • Membrane Lipids