GMI-1070, a novel pan-selectin antagonist, reverses acute vascular occlusions in sickle cell mice

Blood. 2010 Sep 9;116(10):1779-86. doi: 10.1182/blood-2009-12-260513. Epub 2010 May 27.

Abstract

Leukocyte adhesion in the microvasculature influences blood rheology and plays a key role in vaso-occlusive manifestations of sickle cell disease. Notably, polymorphonuclear neutrophils (PMNs) can capture circulating sickle red blood cells (sRBCs) in inflamed venules, leading to critical reduction in blood flow and vaso-occlusion. Recent studies have suggested that E-selectin expression by endothelial cells plays a key role by sending activating signals that lead to the activation of Mac-1 at the leading edge of PMNs, thereby allowing RBC capture. Thus, the inhibition of E-selectin may represent a valuable target in this disease. Here, we have tested the biologic properties of a novel synthetic pan-selectin inhibitor, GMI-1070, with in vitro assays and in a humanized model of sickle cell vaso-occlusion analyzed by intravital microscopy. We have found that GMI-1070 predominantly inhibited E-selectin-mediated adhesion and dramatically inhibited sRBC-leukocyte interactions, leading to improved microcirculatory blood flow and improved survival. These results suggest that GMI-1070 may represent a valuable novel therapeutic intervention for acute sickle cell crises that should be further evaluated in a clinical trial.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acute Disease
  • Anemia, Sickle Cell / metabolism
  • Anemia, Sickle Cell / physiopathology
  • Anemia, Sickle Cell / prevention & control*
  • Animals
  • Blood Flow Velocity / drug effects
  • Cell Adhesion / drug effects
  • Cell Line
  • E-Selectin / metabolism
  • Erythrocytes / cytology
  • Erythrocytes / drug effects
  • Erythrocytes / metabolism
  • Female
  • Glycolipids / chemistry
  • Glycolipids / pharmacology*
  • Hemodynamics / drug effects
  • Humans
  • Kaplan-Meier Estimate
  • L-Selectin / metabolism
  • Leukocyte Rolling / drug effects
  • Leukocytes / cytology
  • Leukocytes / drug effects
  • Leukocytes / metabolism
  • Male
  • Mice
  • Mice, Inbred C57BL
  • P-Selectin / metabolism
  • Selectins / metabolism*
  • Vascular Diseases / metabolism
  • Vascular Diseases / physiopathology
  • Vascular Diseases / prevention & control*

Substances

  • E-Selectin
  • Glycolipids
  • P-Selectin
  • Selectins
  • L-Selectin
  • rivipansel