Abstract
A triene-modified analog of the potent immunosuppressive agent rapamycin was found to be a potent inhibitor of the the peptidyl prolyl cis-trans isomerase activity of human FKBP (K i = 12.5 nM). This analog was not immunosuppressive in a thymocyte proliferation assay itself, but was able to antagonize the effect of rapamycin. This new analog should be useful as a mechanistic probe for macrocyclic immunosuppressants.
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