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Cyclosporin A (CsA) is a tight-binding inhibitor of the peptidyl-prolyl cis/trans isomerase (PPIase) activity of human cytosolic cyclophilin (Cyp18), the putative receptor for immunosuppressive effects of the drug. We examined the influence of cremophor EL (CEL), a surfactant that has found wide use for CsA formulation, on the kinetics of inhibition of the enzyme by CsA. Stock solutions of CsA in...
The cytosolic peptidyl-prolyl cis/trans isomerase cyclophilin from pig kidney can accelerate catalytically the cis/trans isomerization of prolyl peptide bonds. One- and two-dimensional 1 H NMR spectroscopy was used to prove that the polypeptide hormone calcitonin is a substrate for cyclophilin. Isomerization of only one of the two prolyl peptide bonds is catalyzed significantly. The efficiency...
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