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. Author manuscript; available in PMC: 2016 Nov 18.
Published in final edited form as: Nature. 2016 May 18;534(7606):272–276. doi: 10.1038/nature17963

Figure 3. RapaLink-1 is a potent mTOR inhibitor.

Figure 3

a, Molecular model constructed by two available co-crystal structures, mTOR catalytic domain bearing TORKi PP242 (4JT5) and mTOR FRB domain/rapamycin/FKBP12 (1FAP). Dotted line represents a guide line for the linker design of bivalent mTOR inhibitors. b, RapaLink-1 structure is displayed. c, MCF-7 cells were treated with RapaLink-1, -2, and -3 or (d) with rapamycin, MLN0128, combination of rapamycin and MLN0128 or RapaLink-1 for 4 hours followed by immunoblotting. The rapamycin panel is the same shown in Figure 1b and the RapaLink-1 panel is the same shown in Figure 3c. For gel source data, see Supplemental Figure 3.