Identification of cyclophilin as the erythrocyte ciclosporin-binding protein

  • Foxwell B
  • Frazer G
  • Winters M
 et al. 
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Previous studies on the distribution of circulating ciclosporin have shown that the majority of the drug is associated with erythrocytes. In order to investigate the nature of ciclosporin-erythrocyte binding, binding studies were performed on isolated erythrocytes. At therapeutic concentrations (approx. 0.5 μg/ml in whole blood) > 90% of the erythrocyte associated ciclosporin was found in the cytosol The cytosolic binding capacity was approximately (2-2.5) · 105molecules of ciclosporin per cell. A lower affinity binding of the drug to the plasma membrane occurred only at higher ciclosporin concentrations. The ciclosporin-binding species was purified from erythrocyte cytosol using ciclosporin-Affigel affinity chromatography. This revealed a 16 kDa protein, similar in size to the ciclosporin-binding protein, cyclophilin, previously identified in lymphocyte cytosol. Immunochemical analysis using rabbit anti-bovine spleen cyclophilin antisera revealed that the erythrocyte ciclosporin-binding protein was either cyclophilin or a closely related protein. It is concluded that intracellular ciclosporin-binding within erythrocytes is mostly attributable to the presence of a single protein or protein family represented by cyclophilin. The presence of (2-2.5) · 105copies of this binding protein within each erythrocyte is responsible for the ciclosporin found associated with erythrocytes. © 1988.

Author-supplied keywords

  • (Human blood)
  • Affinity binding
  • Ciclosporin
  • Cyclophilin
  • Drug-membrane interaction

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  • Brian M.J. Foxwell

  • Giles Frazer

  • Marijlein Winters

  • Peter Hiestand

  • Roland Wenger

  • Bernhard Ryffel

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