Comparison of binding to peripheral blood lymphocytes between active and inactive derivatives of cyclosporine

P. M. Colombani, E. C. Bright, A. D. Hess

Research output: Contribution to journalArticlepeer-review

3 Scopus citations

Abstract

We have compared the relative binding of active and inactive dansylated derivatives of CsA. We find that there is a significant difference in binding to intact PBL between these drugs. Binding appears saturable, temperature dependent, and is specific for cyclosporines. By removing membrane barriers, we can increase specific binding of the inactive derivative of CsA and CsH. Thus, CsH can become functionally active by removing membrane barriers prior to cell activation. These results indicate that the varied inhibitory activity and apparent stereospecificity of the cyclosporines may, in large part, be explained by their ability to passively partition through the cell membrane. Further studies with other derivatives of CsA and permeabilized PBL should disclose a true rank order of potency fof the cyclosporines and help determine which CsA binding proteins are critically involved in its effect on T lymphocyte activation.

Original languageEnglish (US)
Pages (from-to)46-50
Number of pages5
JournalTransplantation proceedings
Volume20
Issue number2 SUPPL. 2
StatePublished - 1988

ASJC Scopus subject areas

  • Surgery
  • Transplantation

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