Modulating sphingosine-1-phosphate receptors to improve chemotherapy efficacy against Ewing sarcoma

Int J Cancer. 2020 Aug 15;147(4):1206-1214. doi: 10.1002/ijc.32862. Epub 2020 Jan 21.

Abstract

Tumor vasculature is innately dysfunctional. Poorly functional tumor vessels inefficiently deliver chemotherapy to tumor cells; vessel hyper-permeability promotes chemotherapy delivery primarily to a tumor's periphery. Here, we identify a method for enhancing chemotherapy efficacy in Ewing sarcoma (ES) in mice by modulating tumor vessel permeability. Vessel permeability is partially controlled by the G protein-coupled Sphinosine-1-phosphate receptors 1 and 2 (S1PR1 and S1PR2) on endothelial cells. S1PR1 promotes endothelial cell junction integrity while S1PR2 destabilizes it. We hypothesize that an imbalance of S1PR1:S1PR2 is partially responsible for the dysfunctional vascular phenotype characteristic of ES and that by altering the balance in favor of S1PR1, ES vessel hyper-permeability can be reversed. In our study, we demonstrate that pharmacologic activation of S1PR1 by SEW2871 or inhibition of S1PR2 by JTE-013 caused more organized, mature and functional tumor vessels. Importantly, S1PR1 activation or S1PR2 inhibition improved antitumor efficacy. Our data suggests that pharmacologic targeting of S1PR1 and S1PR2 may be a useful adjuvant to standard chemotherapy for ES patients.

Keywords: Ewing sarcoma; S1PR1; S1PR2; chemotherapy efficacy; vascular permeability.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibiotics, Antineoplastic / pharmacology
  • Bone Neoplasms / drug therapy*
  • Bone Neoplasms / metabolism
  • Capillary Permeability / drug effects
  • Cell Line, Tumor
  • Doxorubicin / pharmacology*
  • Endothelial Cells / drug effects
  • Endothelial Cells / metabolism
  • Humans
  • Mice, Nude
  • Oxadiazoles / pharmacology*
  • Pyrazoles / pharmacology*
  • Pyridines / pharmacology*
  • Sarcoma, Ewing / drug therapy*
  • Sarcoma, Ewing / metabolism
  • Sphingosine 1 Phosphate Receptor Modulators / pharmacology
  • Sphingosine-1-Phosphate Receptors / antagonists & inhibitors*
  • Sphingosine-1-Phosphate Receptors / metabolism
  • Thiophenes / pharmacology*
  • Treatment Outcome
  • Xenograft Model Antitumor Assays / methods

Substances

  • Antibiotics, Antineoplastic
  • JTE 013
  • Oxadiazoles
  • Pyrazoles
  • Pyridines
  • S1pr1 protein, mouse
  • SEW2871
  • Sphingosine 1 Phosphate Receptor Modulators
  • Sphingosine-1-Phosphate Receptors
  • Thiophenes
  • sphingosine-1-phosphate receptor-2, mouse
  • Doxorubicin