A Bi-Steric mTORC1-Selective Inhibitor Overcomes Drug Resistance in Breast Cancer

To address which mTOR kinase form was required for the survival of malignant cells, investigators used RMC-6272, a bi-steric molecule with a rapamycin-like moiety linked to an mTOR active-site inhibitor that displayed >25-fold selectivity for mTORC1 over mTORC2 substrates.