Overcoming Resistance to Targeted Anticancer Therapies through Small-Molecule-Mediated MEK Degradation (Cell Chemical Biology)

Rapid onset of resistance to targeted kinase inhibitors limits their use in treating advanced cancers. Peh et al. show that combination of diverse kinase inhibitors with a procaspase-3 activating compound (PAC-1) leads to degradation of MEK1/2, dramatically delaying acquired resistance.