Therapeutic paradigm of dual targeting VEGF and PDGF for effectively treating FGF-2 off-target tumors

Nat Commun. 2020 Jul 24;11(1):3704. doi: 10.1038/s41467-020-17525-6.

Abstract

FGF-2 displays multifarious functions in regulation of angiogenesis and vascular remodeling. However, effective drugs for treating FGF-2+ tumors are unavailable. Here we show that FGF-2 modulates tumor vessels by recruiting NG2+ pricytes onto tumor microvessels through a PDGFRβ-dependent mechanism. FGF-2+ tumors are intrinsically resistant to clinically available drugs targeting VEGF and PDGF. Surprisingly, dual targeting the VEGF and PDGF signaling produces a superior antitumor effect in FGF-2+ breast cancer and fibrosarcoma models. Mechanistically, inhibition of PDGFRβ ablates FGF-2-recruited perivascular coverage, exposing anti-VEGF agents to inhibit vascular sprouting. These findings show that the off-target FGF-2 is a resistant biomarker for anti-VEGF and anti-PDGF monotherapy, but a highly beneficial marker for combination therapy. Our data shed light on mechanistic interactions between various angiogenic and remodeling factors in tumor neovascularization. Optimization of antiangiogenic drugs with different principles could produce therapeutic benefits for treating their resistant off-target cancers.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiogenesis Inhibitors / pharmacology*
  • Animals
  • Biomarkers, Tumor
  • Blood Pressure
  • Breast Neoplasms / drug therapy
  • Breast Neoplasms / pathology
  • Capillary Permeability
  • Cell Proliferation
  • Disease Models, Animal
  • Drug Resistance, Neoplasm / drug effects
  • Drug Therapy, Combination
  • Fibroblast Growth Factor 2 / drug effects*
  • Fibroblast Growth Factor 2 / metabolism*
  • Humans
  • Mice
  • Mice, Inbred C57BL
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Neovascularization, Pathologic / drug therapy
  • Platelet-Derived Growth Factor / drug effects*
  • Platelet-Derived Growth Factor / metabolism
  • Receptor, Platelet-Derived Growth Factor beta
  • Signal Transduction / drug effects
  • Tumor Hypoxia
  • Tumor Microenvironment / drug effects
  • Vascular Endothelial Growth Factor A / drug effects*
  • Vascular Endothelial Growth Factor A / metabolism

Substances

  • Angiogenesis Inhibitors
  • Biomarkers, Tumor
  • Platelet-Derived Growth Factor
  • Vascular Endothelial Growth Factor A
  • Fibroblast Growth Factor 2
  • Receptor, Platelet-Derived Growth Factor beta