Ocain T D, Longhi D, Steffan R J, Caccese R G, Sehgal S N
Wyeth-Ayerst Research, Princeton, NJ 08543.
Biochem Biophys Res Commun. 1993 May 14;192(3):1340-6. doi: 10.1006/bbrc.1993.1563.
A triene-modified analog of the potent immunosuppressive agent rapamycin was found to be a potent inhibitor of the peptidyl prolyl cis-trans isomerase activity of human FKBP (Ki = 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.
