Aflibercept Traps Galectin-1, an Angiogenic Factor Associated with Diabetic Retinopathy

Sci Rep. 2015 Dec 9:5:17946. doi: 10.1038/srep17946.

Abstract

Vascular endothelial growth factor (VEGF)-A-driven angiogenesis contributes to various disorders including cancer and proliferative diabetic retinopathy (PDR). Among several VEGF-A blockers clinically used is aflibercept, a chimeric VEGFR1/VEGFR2-based decoy receptor fused to the Fc fragment of IgG1 (i.e., VEGFR1/VEGFR2-Fc). Here, we revealed a novel anti-angiogenic function for aflibercept beyond its antagonism against VEGF family members. Immunoprecipitation and mass spectrometry analyses identified galectin-1 as an aflibercept-interacting protein. Biolayer interferometry revealed aflibercept binding to galectin-1 with higher affinity than VEGFR1-Fc and VEGFR2-Fc, which was abolished by deglycosylation of aflibercept with peptide:N-glycosidase F. Retinal LGALS1/Galectin-1 mRNA expression was enhanced in vitro by hypoxic stimulation and in vivo by induction of diseases including diabetes. Galectin-1 immunoreactivity co-localized with VEGFR2 in neovascular tissues surgically excised from human eyes with PDR. Compared with non-diabetic controls, intravitreal galectin-1 protein levels were elevated in PDR eyes, showing no correlation with increased VEGF-A levels. Preoperative injection of bevacizumab, a monoclonal antibody to VEGF-A, reduced the VEGF-A, but not galectin-1, levels. Galectin-1 application to human retinal microvascular endothelial cells up-regulated VEGFR2 phosphorylation, which was eliminated by aflibercept. Our present findings demonstrated the neutralizing efficacy of aflibercept against galectin-1, an angiogenic factor associated with PDR independently of VEGF-A.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiogenesis Inducing Agents / metabolism*
  • Cell Line
  • Diabetic Retinopathy / etiology*
  • Diabetic Retinopathy / metabolism*
  • Diabetic Retinopathy / pathology
  • Endothelial Cells / metabolism
  • Galectin 1 / antagonists & inhibitors
  • Galectin 1 / genetics
  • Galectin 1 / metabolism*
  • Gene Expression Regulation / drug effects
  • Humans
  • Protein Binding
  • Protein Interaction Mapping
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Receptors, Vascular Endothelial Growth Factor / metabolism*
  • Receptors, Vascular Endothelial Growth Factor / pharmacology
  • Recombinant Fusion Proteins / metabolism*
  • Recombinant Fusion Proteins / pharmacology
  • Retinal Pigment Epithelium / metabolism
  • Vascular Endothelial Growth Factor A / antagonists & inhibitors
  • Vascular Endothelial Growth Factor A / metabolism
  • Vascular Endothelial Growth Factor Receptor-2 / metabolism

Substances

  • Angiogenesis Inducing Agents
  • Galectin 1
  • RNA, Messenger
  • Recombinant Fusion Proteins
  • Vascular Endothelial Growth Factor A
  • aflibercept
  • Receptors, Vascular Endothelial Growth Factor
  • Vascular Endothelial Growth Factor Receptor-2