Rapamycin comparison with

Andoh TF, Burdmann EA, Fransechini N, Houghton DC, Bennett WM. Comparison of acute rapamycin nephrotoxicity with cyclosporine and FK506. Kidney Int 1996 50 1110-1117. 

Crowe A, Lemaire M. In vitro and in situ absorption of SDZ-RAD using a human intestinal cell line (Caco-2) and a single pass perfusion model in rats comparison with rapamycin. Pharm Res (NY) 1998 15 1666-1672. 

The structures of FKBP12 (in complex with FK506), FKBP25 (in complex with rapamycin), and FKBP52 (the N-terminal domain) are on file at the Brookhaven Protein Data Bank. The protein structures and rotamase domains of these three FKBPs, sans ligands, are depicted in Figure 5 for comparison and reference in the following discussion of the FKBPs. 

The selective mTOR inhibitor OSI-027 (67) from OSI Pharmaceuticals (now Astellas) is undergoing a Phase I clinical trial in patients with advanced solid tumors or lymphoma.123 A comparison study of this compound with rapamycin showed that while the mTORCl inhibitor rapamycin only partially inhibited phosphorylation of 4E-BP1, OSI-027 fully inhibited this process. OSI-027 also proved more effective than rapamycin in induction of apoptosis in a variety of tumor cell lines.124 Other studies demonstrated that OSI-027 is effective in chronic myeloid leukemia (CML) patients with a particular... 

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