Mechanism of action

Mechanism of action describes the process by which a molecule, such as a drug, functions to produce a pharmacological effect. A drug’s mechanism of action may refer to its effects on a biological readout such as cell growth, or its interaction and modulation of its direct biomolecular target, for example a protein or nucleic acid.

Latest Research and Reviews

News and Comment

  • News and Views |

    A new study reveals that, in addition to its longstanding role in recruiting proteins to the proteasome, ubiquitination can also induce a structural destabilization that allows the target protein to be efficiently unraveled for degradation.

    • Cameron G. Roberts
    •  & Jonathan N. Pruneda
  • News and Views |

    Ferroptosis induced by GPX4 inhibition offers promise for killing drug-resistant cancer cells, yet current GPX4 inhibitors lack selectivity. The discovery of masked nitrile oxide electrophiles as selective prodrug inhibitors of GPX4 points to an attractive path for chemically inducing ferroptosis.

    • Stefan G. Kathman
    •  & Benjamin F. Cravatt
  • News and Views |

    The site-specific monoubiquitination of FANCD2 is crucial for the Fanconi anemia DNA repair pathway and tumor suppression. This modification is mediated by the E2 enzyme UBE2T and the E3 ligase FANCL through a novel allosteric mechanism.

    • Koichi Sato
    •  & Puck Knipscheer
  • News and Views |

    Genetic screens uncover a bioactivation pathway for Lasonolide A involving enrichment in lipid droplets and cleavage into a cytotoxic, soluble metabolite by a lipid droplet-associated serine hydrolase. These findings identify enzymatically regulated phase partitioning as a drug activation mechanism.

    • Zhipeng Li
    • , Siti Nur Sarah Morris
    •  & James A. Olzmann
  • News and Views |

    Phenotypic screening is an engine of discovery for bioactive small molecules and can unravel novel mechanisms and pathways controlling cellular physiology. A recent study reveals the CPSF complex as a pharmacologically tractable target of JTE-607 and context-specific cancer dependency.

    • Michael A. Erb