Abstract
In order to establish whether CyP is the pharmacologically relevant CsA receptor, the CyP binding v immunosuppressive activity was measured for an extensive, structurally varied group of CsA analogues. Overall, CyP binding was found to parallel immunosuppressive activity. Other than MeAla6-CsA, the few exceptions to the correlation could be ascribed to cellular metabolism. These results strongly implicate CyP or a related protein in the mechanism of action of cyclosporine.
MeSH terms
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Animals
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Carrier Proteins / metabolism*
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Cyclosporins / metabolism*
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Ethers / pharmacology
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Immunosuppression Therapy*
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Immunosuppressive Agents*
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In Vitro Techniques
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Interleukin-2 / metabolism
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Ionomycin
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Lymphocyte Activation / drug effects*
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Lymphocyte Culture Test, Mixed
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Mice
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Peptidylprolyl Isomerase
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Structure-Activity Relationship
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Tetradecanoylphorbol Acetate / pharmacology
Substances
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Carrier Proteins
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Cyclosporins
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Ethers
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Immunosuppressive Agents
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Interleukin-2
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Ionomycin
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Peptidylprolyl Isomerase
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Tetradecanoylphorbol Acetate