Table 1.
Ternary-complex formation and inhibition of mTOR by FKBP homologs
| Protein | EC50a,b (nM) | IC50a,c (nM) |
|---|---|---|
| FKBP12 | 3.8 ± 0.6 | 0.69 ± 0.17 |
| FKBP12.6 | 5.6 ± 0.9 | 4.79 ± 1.76 |
| FKBP13 | 6.7 ± 1.6 | 2.48 ± 0.82 |
| FKBP25 | 4.3 ± 0.9 | 2.61 ± 0.57 |
| FKBP51 | 25 ± 6.7 | 1.95 ± 0.36 |
| FKBP52 | 25.5 ± 5.8 | 1.68 ± 0.51 |
| FKBP51 FK1 | 10.5 ± 1.8 | |
| FKBP52 FK1 | 26.2 ± 5.6 |
a
The values shown are means and standard deviations.
b
EC50s for ternary GST-FRB/rapamycin/EGFP-FKBP complex formation are shown (see Fig. S1 in the supplemental material).
c
IC50s for inhibition of the kinase activity of purified, truncated mTOR by different FKBP-rapamycin complexes are shown (see Fig. S2 in the supplemental material).