Peripheral vascular disease: preclinical models and emerging therapeutic targeting of the vascular endothelial growth factor ligand-receptor system

Expert Opin Ther Targets. 2021 May;25(5):381-391. doi: 10.1080/14728222.2021.1940139. Epub 2021 Jun 17.

Abstract

Introduction: Vascular endothelial growth factor (VEGF)-A is a sought therapeutic target for PAD treatment because of its potent role in angiogenesis. However, no therapeutic benefit was achieved in VEGF-A clinical trials, suggesting that our understanding of VEGF-A biology and ischemic angiogenic processes needs development. Alternate splicing in VEGF-A produces pro- and anti-angiogenic VEGF-A isoforms; the only difference being a 6-amino acid switch in the C-terminus of the final 8th exon of the gene. This finding has changed our understanding of VEGF-A biology and may explain the lack of benefit in VEGF-A clinical trials. It presents new therapeutic opportunities for peripheral arterial disease (PAD) treatment.Areas covered: Literature search was conducted to include: 1) predicted mechanism by which the anti-angiogenic VEGF-A isoform would inhibit angiogenesis, 2) unexpected mechanism of action, and 3) how this mechanism revealed novel signaling pathways that may enhance future therapeutics in PAD.Expert opinion: Inhibiting a specific anti-angiogenic VEGF-A isoform in ischemic muscle promotes perfusion recovery in preclinical PAD. Additional efforts focused on the production of these isoforms, and the pathways altered by modulating different VEGF receptor-ligand interactions, and how this new data may allow bedside progress offers new approaches to PAD are discussed.I.

Keywords: Endothelium; alternate splicing; angiogenesis; atherosclerotic occlusion; chronic limb ischemia; chronic limb-threatening ischemia; ischemia; macrophage polarization; peripheral artery disease.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Alternative Splicing / genetics
  • Angiogenesis Inhibitors / pharmacology
  • Animals
  • Humans
  • Ligands
  • Molecular Targeted Therapy*
  • Neovascularization, Pathologic / drug therapy
  • Neovascularization, Pathologic / pathology
  • Peripheral Arterial Disease / drug therapy*
  • Peripheral Arterial Disease / physiopathology
  • Protein Isoforms
  • Signal Transduction / drug effects
  • Vascular Endothelial Growth Factor A / antagonists & inhibitors*
  • Vascular Endothelial Growth Factor A / genetics
  • Vascular Endothelial Growth Factor A / metabolism

Substances

  • Angiogenesis Inhibitors
  • Ligands
  • Protein Isoforms
  • VEGFA protein, human
  • Vascular Endothelial Growth Factor A