1. Simulations to guide drug design strategies for anti–Bcl-2 therapy.
Simulations to guide drug design strategies for anti–Bcl-2 therapy. A, minimum amount of therapy required to induce tumor regression is observed to vary exponentially with the inhibition constant KDi of BL193 for Bcl-2. Reducing KDi from its baseline value by 25% decreases the least amount of therapy required from to 0.52 mmol/L. B, as the rate of diffusion Di of BL193 into the cell is increased, the least amount of efficacious therapy reduces by a maximum amount of 56%, after which no significant change is observed when compared with baseline values for Di.
Harsh Vardhan Jain et al. Mol Cancer Ther 2009;8:
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