In conclusion, our findings can be summarized as follows: (1) we synthesized two analogues ([TOAC1, Api4] TG and [Api8] TG), with a perturbed structural sector of the amphipathic helix, that display selective cytotoxicity towards a cancer cell line; (2) a defined ratio between H and μ is required to retain toxicity, therefore these parameters must be taken into account in the design of future TG analogues; (3) the activity is turned off when the binding falls below a critical threshold. The gene discussed is BIRC5; the disease is cancer.