Indeed, several biological studies and clinical evidence demonstrated that the inhibition of Hsp90 helps to overcome resistance to known blockers of B-Raf, and that their combined inhibition provides synergistic effects in different cancer-related contexts.85–88 In line with the polypharmacology concept, further advantages can also be envisioned for cancer treatment on the design of ligands endowed with multi-target activity (Figure 1). The gene discussed is BRAF; the disease is cancer.